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Target
G protein-coupled receptor kinase 5
Ligand
BDBM50191325
Substrate
n/a
Meas. Tech.
ChEMBL_1612831 (CHEMBL3854631)
IC50
631000±n/a nM
Citation
 Guccione, M; Ettari, R; Taliani, S; Da Settimo, F; Zappalą, M; Grasso, S G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives. J Med Chem 59:9277-9294 (2016) [PubMed]  Article 
Target
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:
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHINQCEDLRRTIDRDYCSLCDKQPVGRLLFRQFCETRPGLESYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFITQVGRDLVSQTEEKLLQKPCKELFSACVQSVHDYLRGEPFHEYLDSMYFDRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEKVNSRFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLEDLHHENIVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQRYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSICKMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDIEQFSTVKGVNLDHTDDDFYSKFSTGSVPIPWQSEMIETECFKELNVFGPHGTLSPDLNRSHPPEPPKKGLLQRLFKRQHQNNSKSSPNSKTSFNHHINSNHVSSNSTGSS
  
Inhibitor
Name:
BDBM50191325
Synonyms:
CHEMBL3918278
Type:
Small organic molecule
Emp. Form.:
C26H19F4N5O
Mol. Mass.:
493.4556
SMILES:
CC1=C(C(N=C(N1)c1ccc(cc1)C(F)(F)F)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1 |c:4,t:1|
Structure:
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