Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetG protein-coupled receptor kinase 5
LigandBDBM283996
Substrate/Competitorn/a
Meas. Tech.Assays for Inhibition of GRKs
pH7±n/a
IC50 410±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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM283996
n/a
NameBDBM283996
Synonyms:E22 | US10023564, Example 22
TypeSmall organic molecule
Emp. Form.C25H23FN8O4
Mol. Mass.518.4997
SMILESCCc1nc(CNC(=O)c2cc(ccc2F)C2NC(=O)NC(C)=C2C(=O)Nc2ccc3[nH]ncc3c2)no1 |c:23|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: