Protein kinase G (PKG) 2 | Protein kinase G (PKG) family | IUPHAR/BPS Guide to PHARMACOLOGY

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Protein kinase G (PKG) 2

Target not currently curated in GtoImmuPdb

Target id: 1493

Nomenclature: Protein kinase G (PKG) 2

Abbreviated Name: PKG2

Family: Protein kinase G (PKG) 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 - 762 4q13.1-q21.1 PRKG2 protein kinase cGMP-dependent 2
Mouse - 762 5 Prkg2 protein kinase, cGMP-dependent, type II
Rat - 762 14p22 Prkg2 protein kinase cGMP-dependent 2
Previous and Unofficial Names
CGK 2 | GDPKII | protein kinase cGMP-dependent type 2 | PRKGR2 | protein kinase
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.12

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 Value Parameter Reference
compound 32 [PMID: 20471253] Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.4x10-8 M) [2]
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: 3-4

Key to terms and symbols Click column headers to sort
Target used in screen: PRKG2
Ligand Sp. Type Action Value Parameter
GSK690693 Hs Inhibitor Inhibition 8.5 pKd
staurosporine Hs Inhibitor Inhibition 7.8 pKd
A-674563 Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
midostaurin Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.6 pKd
PP-242 Hs Inhibitor Inhibition 6.3 pKd
ruxolitinib Hs Inhibitor Inhibition 6.2 pKd
KW-2449 Hs Inhibitor Inhibition 6.1 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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/PKG2(PRKG2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
midostaurin Hs Inhibitor Inhibition -9.4
K-252a Hs Inhibitor Inhibition -4.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 2.2
PKR inhibitor Hs Inhibitor Inhibition 3.0
SB 218078 Hs Inhibitor Inhibition 6.0
staurosporine Hs Inhibitor Inhibition 7.1
JAK inhibitor I Hs Inhibitor Inhibition 14.3
indirubin derivative E804 Hs Inhibitor Inhibition 28.1
Gö 6976 Hs Inhibitor Inhibition 28.2
Cdk4 inhibitor Hs Inhibitor Inhibition 29.7
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. 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

Protein kinase G (PKG) family: Protein kinase G (PKG) 2. Last modified on 19/02/2015. Accessed on 15/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1493.