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Target
G protein-coupled receptor kinase 6
Ligand
BDBM50566949
Substrate
n/a
Meas. Tech.
ChEMBL_2102048 (CHEMBL4810444)
IC50
3.8±n/a nM
Citation
 Uehling, DE; Joseph, B; Chung, KC; Zhang, AX; Ler, S; Prakesch, MA; Poda, G; Grouleff, J; Aman, A; Kiyota, T; Leung-Hagesteijn, C; Konda, JD; Marcellus, R; Griffin, C; Subramaniam, R; Abibi, A; Strathdee, CA; Isaac, MB; Al-Awar, R; Tiedemann, 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 Chem 64:11129-11147 (2021) [PubMed]  Article 
Target
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:
MELENIVANTVLLKAREGGGGNRKGKSKKWRQMLQFPHISQCEELRLSLERDYHSLCERQPIGRLLFREFCATRPELSRCVAFLDGVAEYEVTPDDKRKACGRQLTQNFLSHTGPDLIPEVPRQLVTNCTQRLEQGPCKDLFQELTRLTHEYLSVAPFADYLDSIYFNRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKKLEKKRIKKRKGEAMALNEKQILEKVNSRFVVSLAYAYETKDALCLVLTLMNGGDLKFHIYHMGQAGFPEARAVFYAAEICCGLEDLHRERIVYRDLKPENILLDDHGHIRISDLGLAVHVPEGQTIKGRVGTVGYMAPEVVKNERYTFSPDWWALGCLLYEMIAGQSPFQQRKKKIKREEVERLVKEVPEEYSERFSPQARSLCSQLLCKDPAERLGCRGGSAREVKEHPLFKKLNFKRLGAGMLEPPFKPDPQAIYCKDVLDIEQFSTVKGVELEPTDQDFYQKFATGSVPIPWQNEMVETECFQELNVFGLDGSVPPDLDWKGQPPAPPKKGLLQRLFSRQDCCGNCSDSEEELPTRL
  
Inhibitor
Name:
BDBM50566949
Synonyms:
CHEMBL4877302
Type:
Small organic molecule
Emp. Form.:
C22H23ClN6O2
Mol. Mass.:
438.91
SMILES:
CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(OC)c23)n[nH]1
Structure:
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