Reaction Details |
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Target | Rhodopsin kinase GRK1 |
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Ligand | BDBM50566946 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2102043 (CHEMBL4810439) |
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IC50 | 190±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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Rhodopsin kinase GRK1 |
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Name: | Rhodopsin kinase GRK1 |
Synonyms: | G protein-coupled receptor kinase 1 | GRK1 | GRK1_HUMAN | PK | RHOK | Rhodopsin kinase |
Type: | PROTEIN |
Mol. Mass.: | 63520.09 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_774378 |
Residue: | 563 |
Sequence: | MDFGSLETVVANSAFIAARGSFDGSSSQPSRDKKYLAKLKLPPLSKCESLRDSLSLEFES
VCLEQPIGKKLFQQFLQSAEKHLPALELWKDIEDYDTADNDLQPQKAQTILAQYLDPQAK
LFCSFLDEGIVAKFKEGPVEIQDGLFQPLLQATLAHLGQAPFQEYLGSLYFLRFLQWKWL
EAQPMGEDWFLDFRVLGKGGFGEVSACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKK
ILMKVHSRFIVSLAYAFETKADLCLVMTIMNGGDIRYHIYNVNEENPGFPEPRALFYTAQ
IICGLEHLHQRRIVYRDLKPENVLLDNDGNVRISDLGLAVELLDGQSKTKGYAGTPGFMA
PELLQGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKHRIISEPVKYPDKFS
QASKDFCEALLEKDPEKRLGFRDETCDKLRAHPLFKDLNWRQLEAGMLMPPFIPDSKTVY
AKDIQDVGAFSTVKGVAFDKTDTEFFQEFATGNCPIPWQEEMIETGIFGELNVWRSDGQM
PDDMKGISGGSSSSSKSGMCLVS
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BDBM50566946 |
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n/a |
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Name | BDBM50566946 |
Synonyms: | CHEMBL4854871 |
Type | Small organic molecule |
Emp. Form. | C21H22FN7O |
Mol. Mass. | 407.4441 |
SMILES | CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1 |r| |
Structure |
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