Reaction Details |
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Target | G protein-coupled receptor kinase 6 |
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Ligand | BDBM50566942 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2102025 (CHEMBL4810421) |
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IC50 | 230±n/a nM |
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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 Chem64:11129-11147 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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G protein-coupled receptor kinase 6 |
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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
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BDBM50566942 |
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n/a |
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Name | BDBM50566942 |
Synonyms: | CHEMBL4875743 |
Type | Small organic molecule |
Emp. Form. | C19H18F2N8 |
Mol. Mass. | 396.3966 |
SMILES | CCc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc3cccc(F)c23)n[nH]1 |r| |
Structure |
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