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Target id: 1468
Nomenclature: G protein-coupled receptor kinase 4
Abbreviated Name: GRK4
Family: GRK4 subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 578 | 4p16.3 | GRK4 | G protein-coupled receptor kinase 4 | |
Mouse | - | 574 | 5 17.91 cM | Grk4 | G protein-coupled receptor kinase 4 | |
Rat | - | 575 | 14q21 | Grk4 | G protein-coupled receptor kinase 4 |
Previous and Unofficial Names ![]() |
GPRK2L | G protein-coupled receptor kinase 2, groucho gene related | GPRK4 |
Database Links ![]() |
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Alphafold | P32298 (Hs), O70291 (Mm), P70507 (Rn) |
BRENDA | 2.7.11.16 |
ChEMBL Target | CHEMBL5861 (Hs) |
Ensembl Gene | ENSG00000125388 (Hs), ENSMUSG00000052783 (Mm), ENSRNOG00000011847 (Rn) |
Entrez Gene | 2868 (Hs), 14772 (Mm), 59077 (Rn) |
Human Protein Atlas | ENSG00000125388 (Hs) |
KEGG Enzyme | 2.7.11.16 |
KEGG Gene | hsa:2868 (Hs), mmu:14772 (Mm), rno:59077 (Rn) |
OMIM | 137026 (Hs) |
Pharos | P32298 (Hs) |
RefSeq Nucleotide | NM_001004056 (Hs), NM_001080743 (Mm), NM_019497 (Mm), NM_022928 (Rn) |
RefSeq Protein | NP_001004056 (Hs), NP_001074212 (Mm), NP_062370 (Mm), NP_075217 (Rn) |
UniProtKB | P32298 (Hs), O70291 (Mm), P70507 (Rn) |
Wikipedia | GRK4 (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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DiscoveRx KINOMEscan® screen ![]() |
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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: 2,4 |
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Target used in screen: GRK4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
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 |
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Target used in screen: nd/GRK4 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | ||
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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. 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]
4. 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]
GRK4 subfamily: G protein-coupled receptor kinase 4. Last modified on 07/12/2016. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1468.