G protein-coupled receptor kinase 5 | GRK4 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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G protein-coupled receptor kinase 5

Target not currently curated in GtoImmuPdb

Target id: 1469

Nomenclature: G protein-coupled receptor kinase 5

Abbreviated Name: GRK5

Family: GRK4 subfamily

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 - 590 10q24-qter GRK5 G protein-coupled receptor kinase 5
Mouse - 590 19 Grk5 G protein-coupled receptor kinase 5
Rat - 590 1q55 Grk5 G protein-coupled receptor kinase 5
Previous and Unofficial Names
GPRK5
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.16

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 1o [PMID: 24210504] Hs Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 5.9x10-8 M) [2]
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: 1,3

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 Hs Inhibitor Inhibition 20.8 8.0 1.0
Ro-32-0432 Hs Inhibitor Inhibition 56.2
K-252a Hs Inhibitor Inhibition 62.0 40.0 5.0
GF109203X Hs Inhibitor Inhibition 71.6 61.0 9.0
JAK inhibitor I Hs Inhibitor Inhibition 72.9 72.0 66.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 74.3 107.0 77.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 75.6 77.0 30.0
PKR inhibitor Hs Inhibitor Inhibition 81.3 71.0 25.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 82.2 95.0 93.0
SU11652 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 20/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1469.