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G protein-coupled receptor kinase 5

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Target not currently curated in GtoImmuPdb

Target id: 1469

Nomenclature: G protein-coupled receptor kinase 5

Abbreviated Name: GRK5

Family: GRK4 subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 590 10q26.11 GRK5 G protein-coupled receptor kinase 5
Mouse - 590 19 56.52 cM Grk5 G protein-coupled receptor kinase 5
Rat - 590 1q55 Grk5 G protein-coupled receptor kinase 5
Previous and Unofficial Names Click here for help
GPRK5
Database Links Click here for help
Alphafold
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.11.16

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 1o [PMID: 24210504] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 5.9x10-8 M) [2]
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: GRK5/GRK5
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.8 8.0 1.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 56.2
K-252a Small molecule or natural product Hs Inhibitor Inhibition 62.0 40.0 5.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 71.6 61.0 9.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 72.9 72.0 66.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 74.3 107.0 77.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 75.6 77.0 30.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.3 71.0 25.0
PDGF receptor tyrosine kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 82.2 95.0 93.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.7 68.0 33.0
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. Cho SY, Lee BH, Jung H, Yun CS, Ha JD, Kim HR, Chae CH, Lee JH, Seo HW, Oh KS. (2013) Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett, 23 (24): 6711-6. [PMID:24210504]

3. 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]

How to cite this page

GRK4 subfamily: G protein-coupled receptor kinase 5. Last modified on 07/12/2016. Accessed on 21/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1469.