| Reaction Details |
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 | Report a problem with these data |
| Target | Rhodopsin kinase GRK1 |
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| Ligand | BDBM50257340 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1689809 |
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| IC50 | 270±n/a nM |
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| Citation |  Okawa, T; Aramaki, Y; Yamamoto, M; Kobayashi, T; Fukumoto, S; Toyoda, Y; Henta, T; Hata, A; Ikeda, S; Kaneko, M; Hoffman, ID; Sang, BC; Zou, H; Kawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem60:6942-6990 (2017) [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 |
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| Synonyms: | G protein-coupled receptor kinase 1 | GRK1 | GRK1_HUMAN | PK | RHOK | Rhodopsin kinase |
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| Type: | PROTEIN |
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| Mol. Mass.: | 63520.09 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_774378 |
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| Residue: | 563 |
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| Sequence: | MDFGSLETVVANSAFIAARGSFDGSSSQPSRDKKYLAKLKLPPLSKCESLRDSLSLEFES
VCLEQPIGKKLFQQFLQSAEKHLPALELWKDIEDYDTADNDLQPQKAQTILAQYLDPQAK
LFCSFLDEGIVAKFKEGPVEIQDGLFQPLLQATLAHLGQAPFQEYLGSLYFLRFLQWKWL
EAQPMGEDWFLDFRVLGKGGFGEVSACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKK
ILMKVHSRFIVSLAYAFETKADLCLVMTIMNGGDIRYHIYNVNEENPGFPEPRALFYTAQ
IICGLEHLHQRRIVYRDLKPENVLLDNDGNVRISDLGLAVELLDGQSKTKGYAGTPGFMA
PELLQGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKHRIISEPVKYPDKFS
QASKDFCEALLEKDPEKRLGFRDETCDKLRAHPLFKDLNWRQLEAGMLMPPFIPDSKTVY
AKDIQDVGAFSTVKGVAFDKTDTEFFQEFATGNCPIPWQEEMIETGIFGELNVWRSDGQM
PDDMKGISGGSSSSSKSGMCLVS
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| BDBM50257340 |
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| n/a |
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| Name | BDBM50257340 |
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| Synonyms: | CHEMBL4072828 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H21F3N6O2 |
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| Mol. Mass. | 494.4684 |
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| SMILES | FC(F)(F)c1ccccc1CNC(=O)c1cccc(NCc2nnc3-c4ccncc4OCCn23)c1 |
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| Structure | 
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