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TargetG protein-coupled receptor kinase 5
LigandBDBM22416
Substrate/Competitorn/a
Meas. Tech.ChEBML_1692746
IC50>100000±n/a nM
Citation Waldschmidt, HVHoman, KTCato, MCCruz-Rodríguez, OCannavo, AWilson, MWSong, JCheung, JYKoch, WJTesmer, JJLarsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem60:3052-3069 (2017) [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 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:
BDBM22416
n/a
NameBDBM22416
Synonyms:(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | (3S,4R)-3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | CHEMBL490 | PAROXETINE | US09969700, Paroxetine | US9944618, Compound ID No. 182 | [3H]Paroxetine
Typeradiolabeled ligand
Emp. Form.C19H20FNO3
Mol. Mass.329.3654
SMILESFc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1
Structure
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