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TargetG protein-coupled receptor kinase 6
LigandBDBM50566937
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2102025 (CHEMBL4810421)
IC50 70±n/a nM
Citation Uehling, DEJoseph, BChung, KCZhang, AXLer, SPrakesch, MAPoda, GGrouleff, JAman, AKiyota, TLeung-Hagesteijn, CKonda, JDMarcellus, RGriffin, CSubramaniam, RAbibi, AStrathdee, CAIsaac, MBAl-Awar, RTiedemann, RE Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma. J Med Chem64:11129-11147 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
G protein-coupled receptor kinase 6
Name:G protein-coupled receptor kinase 6
Synonyms:GPRK6 | GRK6 | GRK6_HUMAN
Type:PROTEIN
Mol. Mass.:66001.83
Organism:Homo sapiens (Human)
Description:ChEMBL_793895
Residue:576
Sequence:
MELENIVANTVLLKAREGGGGNRKGKSKKWRQMLQFPHISQCEELRLSLERDYHSLCERQ
PIGRLLFREFCATRPELSRCVAFLDGVAEYEVTPDDKRKACGRQLTQNFLSHTGPDLIPE
VPRQLVTNCTQRLEQGPCKDLFQELTRLTHEYLSVAPFADYLDSIYFNRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKKLEKKRIKKRKGEAMALNEKQILEK
VNSRFVVSLAYAYETKDALCLVLTLMNGGDLKFHIYHMGQAGFPEARAVFYAAEICCGLE
DLHRERIVYRDLKPENILLDDHGHIRISDLGLAVHVPEGQTIKGRVGTVGYMAPEVVKNE
RYTFSPDWWALGCLLYEMIAGQSPFQQRKKKIKREEVERLVKEVPEEYSERFSPQARSLC
SQLLCKDPAERLGCRGGSAREVKEHPLFKKLNFKRLGAGMLEPPFKPDPQAIYCKDVLDI
EQFSTVKGVELEPTDQDFYQKFATGSVPIPWQNEMVETECFQELNVFGLDGSVPPDLDWK
GQPPAPPKKGLLQRLFSRQDCCGNCSDSEEELPTRL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50566937
n/a
NameBDBM50566937
Synonyms:CHEMBL4850937
TypeSmall organic molecule
Emp. Form.C21H21ClN6
Mol. Mass.392.885
SMILESCCc1cc(Nc2nc(N[C@@H](C)c3ccc(Cl)cc3)nc3ccccc23)n[nH]1 |r|
Structure
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