Top ▲

phosphorylase kinase catalytic subunit gamma 1

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2145

Nomenclature: phosphorylase kinase catalytic subunit gamma 1

Abbreviated Name: PHKG1

Family: Phosphorylase kinase (PHK) family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 387 7p11.2 PHKG1 phosphorylase kinase catalytic subunit gamma 1
Mouse - 388 5 68.26 cM Phkg1 phosphorylase kinase gamma 1
Rat - 388 12q13 Phkg1 phosphorylase kinase catalytic subunit gamma 1
Previous and Unofficial Names Click here for help
gamma phosphorylase kinase | HK-gamma-M | PHKIN01 | phosphorylase kinase, gamma 1 (muscle) | phosphorylase kinase gamma subunit 1 | phosphorylase kinase
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.11.19

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
A-443654 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition - - 3
[3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
A-443654 inhibits PHKG1 activity by approximately 76% using 1μM compound [3].
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: PHKG1
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 9.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
dovitinib Small molecule or natural product 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 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/PHKg1
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 1.2
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.4
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.8
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.3
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 2.7
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.2
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.1
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 7.7
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 8.1
alsterpaullone Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Glycogen storage disease due to muscle phosphorylase kinase deficiency
Synonyms: Glycogen storage disease IX [Disease Ontology: DOID:0050594]
Disease Ontology: DOID:0050594
Orphanet: ORPHA715

References

Show »

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. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation. Nat Chem Biol, 5 (7): 484-93. [PMID:19465931]

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

Phosphorylase kinase (PHK) family: phosphorylase kinase catalytic subunit gamma 1. Last modified on 30/03/2016. Accessed on 08/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2145.