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Target
G protein-coupled receptor kinase 5
Ligand
BDBM50235817
Substrate
n/a
Meas. Tech.
ChEMBL_1658097 (CHEMBL4007709)
IC50
>10000±n/a nM
Citation
 Hoemann, M; Wilson, N; Argiriadi, M; Banach, D; Burchat, A; Calderwood, D; Clapham, B; Cox, P; Duignan, DB; Konopacki, D; Somal, G; Vasudevan, A Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. Bioorg Med Chem Lett 26:5562-5567 (2016) [PubMed]  Article 
Target
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:
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQPIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQVGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEKVNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLEDLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQRYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSICKMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDIEQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRNHPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
  
Inhibitor
Name:
BDBM50235817
Synonyms:
CHEMBL4078893
Type:
Small organic molecule
Emp. Form.:
C18H17ClF3N5O2
Mol. Mass.:
427.808
SMILES:
FC(F)(F)CNc1nc(Nc2ccc(N3CCOCC3)c(Cl)c2)nc2ccoc12
Structure:
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