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G protein-coupled receptor kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 1465

Nomenclature: G protein-coupled receptor kinase 1

Abbreviated Name: GRK1

Family: Opsin/rhodopsin kinases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 563 13q34 GRK1 G protein-coupled receptor kinase 1
Mouse - 564 8 A1.1 Grk1 G protein-coupled receptor kinase 1
Rat - 564 16q12.5 Grk1 G protein-coupled receptor kinase 1
Previous and Unofficial Names Click here for help
Rhodopsin kinase | RK | GPRK1 | RHOK
Database Links Click here for help
Alphafold Q15835 (Hs), Q9WVL4 (Mm), Q63651 (Rn)
BRENDA 2.7.11.14
ChEMBL Target CHEMBL5607 (Hs)
Ensembl Gene ENSG00000185974 (Hs), ENSMUSG00000031450 (Mm), ENSRNOG00000018430 (Rn)
Entrez Gene 6011 (Hs), 24013 (Mm), 81760 (Rn)
Human Protein Atlas ENSG00000185974 (Hs)
KEGG Enzyme 2.7.11.14
KEGG Gene hsa:6011 (Hs), mmu:24013 (Mm), rno:81760 (Rn)
OMIM 180381 (Hs)
Orphanet ORPHA122286 (Hs)
Pharos Q15835 (Hs)
RefSeq Nucleotide NM_002929 (Hs), NM_011881 (Mm), NM_031096 (Rn)
RefSeq Protein NP_002920 (Hs), NP_036011 (Mm), NP_112358 (Rn)
UniProtKB Q15835 (Hs), Q9WVL4 (Mm), Q63651 (Rn)
Wikipedia GRK1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.14

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
balanol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 2
⤷ pIC50 6.5 (IC50 3.4x10-7 M) [2]
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: GRK1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 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
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Oguchi disease 2
OMIM: 613411
Orphanet: ORPHA75382

References

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1. 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]

2. 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]

3. 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 1. Last modified on 10/04/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1465.