p21 (RAC1) activated kinase 5 | PAKB subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

p21 (RAC1) activated kinase 5

Target id: 2138

Nomenclature: p21 (RAC1) activated kinase 5

Abbreviated Name: PAK5

Family: PAKB subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for p21 (RAC1) activated kinase 5 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 719 20p12 PAK5 p21 (RAC1) activated kinase 5
Mouse - 719 2 F3 Pak7 p21 (RAC1) activated kinase 7
Rat - 718 3 q36 Pak7 p21 (RAC1) activated kinase 7
Previous and Unofficial Names
p21 (CDKN1A)-activated kinase 7 | p21-activated kinase 5 | PAK7 | p21 protein (Cdc42/Rac)-activated kinase 7
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure Of The Human P21-Activated Kinase 5
PDB Id:  2F57
Resolution:  1.8Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 4 [PMID: 24432870] Hs Inhibition 7.4 pIC50 6
pIC50 7.4 (IC50 3.6x10-8 M) [6]
GSK690693 Hs Inhibition 7.3 pIC50 5
pIC50 7.3 (IC50 5.2x10-8 M) [5]
PF-3758309 Hs Inhibition 6.8 pIC50 6
pIC50 6.8 (IC50 1.71x10-7 M) [6]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: PAK7
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 8.9 pKd
GSK690693 Hs Inhibitor Inhibition 8.1 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
tamatinib Hs Inhibitor Inhibition 7.2 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.4 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.4 pKd
PP-242 Hs Inhibitor Inhibition 6.3 pKd
sunitinib Hs Inhibitor Inhibition 6.2 pKd
A-674563 Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: PAK5/PAK5
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 2.3 1.0 0.5
K-252a Hs Inhibitor Inhibition 24.5 6.0 1.0
Gö 6976 Hs Inhibitor Inhibition 37.1 12.0 14.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 43.8 9.0 1.0
aminopurvalanol A Hs Inhibitor Inhibition 44.3 57.0 12.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 49.1 43.0 3.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 53.1 21.0 3.0
Syk inhibitor II Hs Inhibitor Inhibition 57.3 48.0 9.0
SU11652 Hs Inhibitor Inhibition 58.9 30.0 8.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 60.3 16.0 7.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S. (2007) Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs. Structure, 15 (2): 201-13. [PMID:17292838]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW et al.. (2008) Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J. Med. Chem., 51 (18): 5663-79. [PMID:18800763]

6. Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I et al.. (2015) Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett, 6 (7): 776-81. [PMID:26191365]

7. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

PAKB subfamily: p21 (RAC1) activated kinase 5. Last modified on 03/12/2015. Accessed on 13/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2138.