G protein-coupled receptor kinase 7 | Opsin/rhodopsin kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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G protein-coupled receptor kinase 7

Target not currently curated in GtoImmuPdb

Target id: 1471

Nomenclature: G protein-coupled receptor kinase 7

Abbreviated Name: GRK7

Family: Opsin/rhodopsin kinases

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 - 553 3q24 GRK7 G protein-coupled receptor kinase 7
Previous and Unofficial Names
GPRK7
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: 2.7.11.14
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
balanol Hs Inhibition 6.7 pIC50 4
pIC50 6.7 (IC50 1.8x10-7 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: GRK7
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.1 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
midostaurin Hs Inhibitor Inhibition 7.3 pKd
PHA-665752 Hs Inhibitor Inhibition 7.2 pKd
sunitinib Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.4 pKd
GSK690693 Hs Inhibitor Inhibition 6.4 pKd
SU-14813 Hs Inhibitor Inhibition 6.3 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.3 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: GRK7/GRK7
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.7 0.5 2.5
K-252a Hs Inhibitor Inhibition 4.9 4.0 4.0
midostaurin Hs Inhibitor Inhibition 15.5 8.0 3.0
Syk inhibitor Hs Inhibitor Inhibition 20.9 14.0 6.0
Gö 6976 Hs Inhibitor Inhibition 37.9 16.0 34.0
Ro-32-0432 Hs Inhibitor Inhibition 40.0
SB 218078 Hs Inhibitor Inhibition 53.4 109.0 105.0
GF109203X Hs Inhibitor Inhibition 60.4 58.0 7.0
JAK inhibitor I Hs Inhibitor Inhibition 60.5 42.0 43.0
SU11652 Hs Inhibitor Inhibition 62.2 57.0 9.0
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. 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. 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]

4. Tesmer JJ, Tesmer VM, Lodowski DT, Steinhagen H, Huber J. (2010) Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J. Med. Chem., 53 (4): 1867-70. [PMID:20128603]

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

Opsin/rhodopsin kinases: G protein-coupled receptor kinase 7. Last modified on 17/02/2015. Accessed on 26/01/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1471.