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TargetG protein-coupled receptor kinase 5
LigandBDBM3149
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1612807 (CHEMBL3854607)
IC50 440±n/a nM
Citation Guccione, MEttari, RTaliani, SDa Settimo, FZappalą, MGrasso, S G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives. J Med Chem59:9277-9294 (2016) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
G protein-coupled receptor kinase 5
Name:G protein-coupled receptor kinase 5
Synonyms:G protein-coupled receptor kinase 5 | G protein-coupled receptor kinase GRK5 | GPRK5 | GRK5 | GRK5_BOVIN
Type:PROTEIN
Mol. Mass.:67903.06
Organism:Bos taurus
Description:ChEMBL_116955
Residue:590
Sequence:
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHINQCEDLRRTIDRDYCSLCDKQ
PVGRLLFRQFCETRPGLESYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFITQ
VGRDLVSQTEEKLLQKPCKELFSACVQSVHDYLRGEPFHEYLDSMYFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSRFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHHENIVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVPIPWQSEMIETECFKELNVFGPHGTLSPDLNRS
HPPEPPKKGLLQRLFKRQHQNNSKSSPNSKTSFNHHINSNHVSSNSTGSS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM3149
n/a
NameBDBM3149
Synonyms:2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid | Acyclic Balanol Analog (-)-1 | Balanol analog 1 | Balanol, 1 | CHEMBL60254
TypeSmall organic molecule
Emp. Form.C28H26N2O10
Mol. Mass.550.5134
SMILESOC(=O)c1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)O[C@@H]1CCCNC[C@H]1NC(=O)c1ccc(O)cc1 |r|
Structure
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