Skip to content
TargetEnzymes

Serine/threonine-protein kinase PAK 4

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
4
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

PAK4_HUMANPAK4Homo sapiens

Serine/threonine-protein kinase PAK 4

Serine/threonine-protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell adhesion turnover, cell migration, growth, proliferation or cell survival26598620. Activation by various effectors including growth factor receptors or active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates and inactivates the protein phosphatase SSH1, leading to increased inhibitory phosphorylation of the actin binding/depolymerizing factor cofilin. Decreased cofilin activity may lead to stabilization of actin filaments. Phosphorylates LIMK1, a kinase that also inhibits the activity of cofilin. Phosphorylates integrin beta5/ITGB5 and thus regulates cell motility. Phosphorylates ARHGEF2 and activates the downstream target RHOA that plays a role in the regulation of assembly of focal adhesions and actin stress fibers. Stimulates cell survival by phosphorylating the BCL2 antagonist of cell death BAD. Alternatively, inhibits apoptosis by preventing caspase-8 binding to death domain receptors in a kinase independent manner. Plays a role in cell-cycle progression by controlling levels of the cell-cycle regulatory protein CDKN1A and by phosphorylating RAN. Promotes kinase-independent stabilization of RHOU, thereby contributing to focal adhesion disassembly during cell migration26598620

Quoted from UniProt’s FUNCTION annotation for O96013 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
CDC420.9990.9020.9000.946
RAC30.9930.9330.9000.116
LIMK10.9680.3170.9000.568
ARHGEF70.9640.1130.9000.627
ARHGEF60.9640.1130.9000.630
RHOU0.9600.4850.5000.854
RAC20.9530.3640.9000.308
RAF10.9490.0710.9000.463
LIMK20.9430.0760.9000.436
INKA10.9420.6800.0000.826

Where it sits in the cell

  • Plasma membrane
  • Cell Junctions

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Serine/threonine-protein kinase PAK 4EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061162
Serine/threonine-protein kinase PAK 4EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061162
Serine/threonine-protein kinase PAK 4EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061162
Serine/threonine-protein kinase PAK 4EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061162