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Protein kinase G (PKG) 2

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Target not currently curated in GtoImmuPdb

Target id: 1493

Nomenclature: Protein kinase G (PKG) 2

Abbreviated Name: PKG2

Family: Protein kinase G (PKG) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 762 4q21.21 PRKG2 protein kinase cGMP-dependent 2
Mouse - 762 5 48.35 cM Prkg2 protein kinase, cGMP-dependent, type II
Rat - 762 14p22 Prkg2 protein kinase cGMP-dependent 2
Previous and Unofficial Names Click here for help
CGK 2 | GDPKII | protein kinase cGMP-dependent type 2 | PRKGR2 | protein kinase
Database Links Click here for help
Alphafold Q13237 (Hs), Q61410 (Mm), Q64595 (Rn)
BRENDA 2.7.11.12
CATH/Gene3D 2.60.120.10
ChEMBL Target CHEMBL2896 (Hs)
Ensembl Gene ENSG00000138669 (Hs), ENSMUSG00000029334 (Mm), ENSRNOG00000002361 (Rn)
Entrez Gene 5593 (Hs), 19092 (Mm), 25523 (Rn)
Human Protein Atlas ENSG00000138669 (Hs)
KEGG Enzyme 2.7.11.12
KEGG Gene hsa:5593 (Hs), mmu:19092 (Mm), rno:25523 (Rn)
OMIM 601591 (Hs)
Pharos Q13237 (Hs)
RefSeq Nucleotide NM_006259 (Hs), NM_008926 (Mm), NM_013012 (Rn)
RefSeq Protein NP_006250 (Hs), NP_032952 (Mm), NP_037144 (Rn)
UniProtKB Q13237 (Hs), Q61410 (Mm), Q64595 (Rn)
Wikipedia PRKG2 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.12

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 7.6 pIC50 2
⤷ pIC50 7.6 (IC50 2.4x10-8 M) [2]
aplithianine A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 4
⤷ pIC50 7.5 (IC50 3.4x10-8 M) [4]
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: PRKG2
Ligand Sp. Type Action Value Parameter
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
KW-2449 Small molecule or natural product 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 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
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 Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition -9.4
K-252a Small molecule or natural product Hs Inhibitor Inhibition -4.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 2.2
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 6.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 14.3
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 28.1
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 28.2
Cdk4 inhibitor Small molecule or natural product 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. Du L, Wilson BAP, Li N, Shah R, Dalilian M, Wang D, Smith EA, Wamiru A, Goncharova EI, Zhang P et al.. (2023) Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases. J Nat Prod, 86 (10): 2283-2293. [PMID:37843072]

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]

How to cite this page

Protein kinase G (PKG) family: Protein kinase G (PKG) 2. Last modified on 11/01/2024. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1493.