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TargetG protein-coupled receptor kinase 5
LigandBDBM50173315
Substrate/Competitorn/a
Meas. Tech.Assays for Inhibition of GRKs
pH7±n/a
IC50 800±n/a nM
Commentsextracted
Citation Larsen, SDHoman, KWaldschmidt, HTesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent US10023564 Publication Date 7/17/2018
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
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  Blast E-value cutoff:
BDBM50173315
n/a
NameBDBM50173315
Synonyms:CHEMBL3809100 | US10023564, Example 4
TypeSmall organic molecule
Emp. Form.C27H22F2N6O3
Mol. Mass.516.4988
SMILESCC1=C(C(NC(=O)N1)c1ccc(F)c(c1)C(=O)NCc1cccc(F)c1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure
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