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protein kinase N2

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Target not currently curated in GtoImmuPdb

Target id: 1521

Nomenclature: protein kinase N2

Abbreviated Name: PKN2

Family: Protein kinase N (PKN) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 984 1p22.2 PKN2 protein kinase N2
Mouse - 983 3 66.69 cM Pkn2 protein kinase N2
Rat - 985 2q44 Pkn2 protein kinase N2
Previous and Unofficial Names Click here for help
PRK2 | PRKCL2 | cardiolipin-activated protein kinase Pak2 | protein kinase C-like 2 | PKN gamma | protease-activated kinase 2 | Stk7
Database Links Click here for help
Alphafold Q16513 (Hs), Q8BWW9 (Mm), O08874 (Rn)
BRENDA 2.7.11.13
CATH/Gene3D 2.60.40.150
ChEMBL Target CHEMBL3032 (Hs)
Ensembl Gene ENSG00000065243 (Hs), ENSMUSG00000004591 (Mm), ENSRNOG00000011317 (Rn)
Entrez Gene 5586 (Hs), 109333 (Mm), 207122 (Rn)
Human Protein Atlas ENSG00000065243 (Hs)
KEGG Enzyme 2.7.11.13
KEGG Gene hsa:5586 (Hs), mmu:109333 (Mm), rno:207122 (Rn)
OMIM 602549 (Hs)
Pharos Q16513 (Hs)
RefSeq Nucleotide NM_006256 (Hs), NM_178654 (Mm), NM_001105755 (Rn)
RefSeq Protein NP_006247 (Hs), NP_848769 (Mm), NP_001099225 (Rn)
UniProtKB Q16513 (Hs), Q8BWW9 (Mm), O08874 (Rn)
Wikipedia PKN2 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.13

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 32 [PMID: 20471253] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 2
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [2]
Y27632 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 6
⤷ pIC50 7.2 (IC50 7x10-8 M) [6]
DiscoveRx KINOMEscan® screen Click here for help
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: 3,5
Key to terms and symbols Click column headers to sort
Target used in screen: PKN2
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.7 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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: PRK2/PKN2(PRK2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 2.4 1.0 1.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.0 1.0 1.5
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 11.4 2.0 1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 15.9 47.0 25.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 19.1 5.0 2.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 44.1 4.0 2.0
Y27632 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 59.7 16.0 4.0
AG 1024 Small molecule or natural product Hs Inhibitor Inhibition 64.3 104.0 117.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.1 29.0 39.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.7 11.0 10.0
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. Bosanac T, Hickey ER, Ginn J, Kashem M, Kerr S, Kugler S, Li X, Olague A, Schlyer S, Young ER. (2010) Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines. Bioorg Med Chem Lett, 20 (12): 3746-9. [PMID:20471253]

3. 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]

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. 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]

6. Wu F, Büttner FH, Chen R, Hickey E, Jakes S, Kaplita P, Kashem MA, Kerr S, Kugler S, Paw Z et al.. (2010) Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. Bioorg Med Chem Lett, 20 (11): 3235-9. [PMID:20462760]

How to cite this page

Protein kinase N (PKN) family: protein kinase N2. Last modified on 19/02/2015. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1521.