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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 ![]() |
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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 ![]() |
GPRK5 |
Database Links ![]() |
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Alphafold | P34947 (Hs), Q8VEB1 (Mm), Q62833 (Rn) |
BRENDA | 2.7.11.16 |
ChEMBL Target | CHEMBL5678 (Hs), CHEMBL3721302 (Mm) |
Ensembl Gene | ENSG00000198873 (Hs), ENSMUSG00000003228 (Mm), ENSRNOG00000011439 (Rn) |
Entrez Gene | 2869 (Hs), 14773 (Mm), 59075 (Rn) |
Human Protein Atlas | ENSG00000198873 (Hs) |
KEGG Enzyme | 2.7.11.16 |
KEGG Gene | hsa:2869 (Hs), mmu:14773 (Mm), rno:59075 (Rn) |
OMIM | 600870 (Hs) |
Pharos | P34947 (Hs) |
RefSeq Nucleotide | NM_005308 (Hs), NM_018869 (Mm), NM_030829 (Rn) |
RefSeq Protein | NP_005299 (Hs), NP_061357 (Mm), NP_110456 (Rn) |
UniProtKB | P34947 (Hs), Q8VEB1 (Mm), Q62833 (Rn) |
Wikipedia | GRK5 (Hs) |
Enzyme Reaction ![]() |
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||
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EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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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 |
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Target used in screen: GRK5/GRK5 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
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]
GRK4 subfamily: G protein-coupled receptor kinase 5. Last modified on 07/12/2016. Accessed on 19/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1469.