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Target id: 1465
Nomenclature: G protein-coupled receptor kinase 1
Abbreviated Name: GRK1
Family: Opsin/rhodopsin kinases
Gene and Protein Information ![]() |
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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 ![]() |
Rhodopsin kinase | RK | GPRK1 | RHOK |
Database Links ![]() |
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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 ![]() |
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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: 1,3 |
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Target used in screen: GRK1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Clinically-Relevant Mutations and Pathophysiology ![]() |
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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]
Opsin/rhodopsin kinases: G protein-coupled receptor kinase 1. Last modified on 10/04/2015. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1465.