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TargetG protein-coupled receptor kinase 5
LigandBDBM50566207
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2094566 (CHEMBL4775829)
IC50 130±n/a nM
Citation Rowlands, RAChen, QBouley, RAAvramova, LVTesmer, JJGWhite, AD Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem64:566-585 (2021) [PubMed]  Article
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 GRK5 | GPRK5 | GRK5 | GRK5_HUMAN
Type:PROTEIN
Mol. Mass.:67798.93
Organism:Homo sapiens (Human)
Description:ChEMBL_1280627
Residue:590
Sequence:
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQ
PIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQ
VGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRN
HPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50566207
n/a
NameBDBM50566207
Synonyms:CHEMBL4777196
TypeSmall organic molecule
Emp. Form.C25H24ClN5O3
Mol. Mass.477.943
SMILESC[C@@H](NC(=O)c1ccc2NC(=O)\C(=C/c3[nH]c(C)c(NC(=O)CCl)c3C)c2c1)c1ccncc1 |r|
Structure
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