Target name

O96013: Serine/threonine-protein kinase PAK 4


  Protein function

Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, growth, proliferation or cell survival. 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.

  Database links

Uniprot primary ID O96013
PDB ID 4APP 4O0Y 4O0X 4O0V 5BMS 4JDJ 4JDK 4JDH 4JDI 2OV2 2BVA 2X4Z 2J0I 4FIE 4FIG 4FIF 4FII 4FIH 4FIJ 4L67 2Q0N 2CDZ 4NJD
DrugBank ID
BioGrid ID 115586
GuidetoPHARMACOLOGY ID 2136
PharmGKB ID PA32920
KEGG ID hsa:10298
DIP ID DIP-39742N
STRING ID 9606.ENSP00000351049
IntAct ID O96013
DMDM
BRENDA 2.7.11.1
Reactome R-HSA-428540
SignaLink O96013
BioCyc
Entrez Gene (Gene ID) 10298
BindingDB O96013

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.617 0.005 1.000 0.000 0.810 0.000 0.767 0.005 0.937 0.005 0.670 0.000 Download
Estate fingerprints 0.838 0.014 0.880 0.009 0.859 0.007 0.856 0.005 0.930 0.000 0.721 0.010 Download
MACCS fingerprints 0.838 0.014 0.924 0.006 0.881 0.007 0.876 0.011 0.955 0.005 0.767 0.018 Download
Daylight fingerprints 0.640 0.000 0.960 0.000 0.800 0.000 0.760 0.000 0.844 0.005 0.625 0.005 Download
ECFP2 fingerprints 0.828 0.012 0.984 0.005 0.906 0.005 0.900 0.009 0.974 0.005 0.826 0.013 Download
ECFP4 fingerprints 0.836 0.005 1.000 0.003 0.919 0.003 0.910 0.000 0.973 0.005 0.845 0.005 Download
ECFP6 fingerprints 0.841 0.003 0.999 0.003 0.920 0.000 0.911 0.003 0.963 0.005 0.851 0.003 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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