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TargetG protein-coupled receptor kinase 5
LigandBDBM50173322
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1581285
IC50>100000±n/a nM
Citation Waldschmidt, HVHoman, KTCruz-Rodríguez, OCato, MCWaninger-Saroni, JLarimore, KMCannavo, ASong, JCheung, JYKirchhoff, PDKoch, WJTesmer, JJLarsen, SD Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem59:3793-807 (2016) [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
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:
BDBM50173322
NameBDBM50173322
Synonyms:CHEMBL3809584
TypeSmall organic molecule
Emp. Form.C30H29FN6O3
Mol. Mass.540.5881
SMILESCN(C(=O)C1=C(C)NC(=O)NC1c1ccc(F)c(c1)C(=O)NCc1c(C)cccc1C)c1ccc2[nH]ncc2c1 |c:4|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a