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Target
G protein-coupled receptor kinase 5
Ligand
BDBM14052
Substrate
n/a
Meas. Tech.
ChEMBL_1612831 (CHEMBL3854631)
IC50
63100±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:
BDBM14052
Synonyms:
N-(1H-indazol-5-yl)-2-methyl-4-(naphthalen-2-yl)-6-oxo-1,4,5,6-tetrahydropyridine-3-carboxamide | dihydropyridone indazole amide 12
Type:
Small organic molecule
Emp. Form.:
C24H20N4O2
Mol. Mass.:
396.4412
SMILES:
CC1=C(C(CC(=O)N1)c1ccc2ccccc2c1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure:
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