protein kinase N2 | Protein kinase N (PKN) family | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase N2

Target not currently curated in GtoImmuPdb

Target id: 1521

Nomenclature: protein kinase N2

Abbreviated Name: PKN2

Family: Protein kinase N (PKN) family

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 984 1p22 PKN2 protein kinase N2
Mouse - 983 3 Pkn2 protein kinase N2
Rat - 983 2q44 Pkn2 protein kinase N2
Previous and Unofficial Names
PRK2 | PRKCL2 | cardiolipin-activated protein kinase Pak2 | protein kinase C-like 2 | PKN gamma | protease-activated kinase 2 | Stk7
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 32 [PMID: 20471253] Hs Inhibition 7.8 pIC50 2
pIC50 7.8 (IC50 1.4x10-8 M) [2]
Y27632 Hs Inhibition 7.2 pIC50 6
pIC50 7.2 (IC50 7x10-8 M) [6]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
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 Hs Inhibitor Inhibition 8.7 pKd
staurosporine Hs Inhibitor Inhibition 8.6 pKd
midostaurin Hs Inhibitor Inhibition 7.8 pKd
A-674563 Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.2 pKd
KW-2449 Hs Inhibitor Inhibition 6.1 pKd
tofacitinib Hs Inhibitor Inhibition 5.9 pKd
sunitinib Hs Inhibitor Inhibition 5.9 pKd
ruboxistaurin 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
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.

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 Hs Inhibitor Inhibition 2.4 1.0 1.0
staurosporine Hs Inhibitor Inhibition 3.0 1.0 1.5
midostaurin Hs Inhibitor Inhibition 11.4 2.0 1.0
SB 218078 Hs Inhibitor Inhibition 15.9 47.0 25.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 19.1 5.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 44.1 4.0 2.0
Y27632 Hs Inhibitor Inhibition 59.7 16.0 4.0
AG 1024 Hs Inhibitor Inhibition 64.3 104.0 117.0
JAK inhibitor I Hs Inhibitor Inhibition 67.1 29.0 39.0
Gö 6976 Hs Inhibitor Inhibition 67.7 11.0 10.0
Displaying the top 10 most potent ligands  View all ligands in screen »


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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 11/08/2020. IUPHAR/BPS Guide to PHARMACOLOGY,