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Target
G protein-coupled receptor kinase 5
Ligand
BDBM50260129
Substrate
n/a
Meas. Tech.
ChEBML_1692746
IC50
42300±n/a nM
Citation
 Waldschmidt, HV; Homan, KT; Cato, MC; Cruz-Rodríguez, O; Cannavo, A; Wilson, MW; Song, J; Cheung, JY; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem 60:3052-3069 (2017) [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:
BDBM50260129
Synonyms:
CHEMBL4098656
Type:
Small organic molecule
Emp. Form.:
C29H31FN2O4
Mol. Mass.:
490.5658
SMILES:
Cc1cccc(C)c1CNC(=O)c1cc(ccc1F)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1 |r|
Structure:
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