Reaction Details |
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Target | G protein-coupled receptor kinase 5 |
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Ligand | BDBM50260130 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1692746 |
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IC50 | 38400±n/a nM |
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Citation | Waldschmidt, HV; Homan, KT; Cato, MC; Cruz-Rodríguez, O; Cannavo, A; Wilson, MW; Song, J; Cheung, JY; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem60:3052-3069 (2017) [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 5 |
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Name: | G protein-coupled receptor kinase 5 |
Synonyms: | G protein-coupled receptor kinase 5 | G protein-coupled receptor kinase GRK5 | GPRK5 | GRK5 | GRK5_BOVIN |
Type: | PROTEIN |
Mol. Mass.: | 67903.06 |
Organism: | Bos taurus |
Description: | ChEMBL_116955 |
Residue: | 590 |
Sequence: | MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHINQCEDLRRTIDRDYCSLCDKQ
PVGRLLFRQFCETRPGLESYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFITQ
VGRDLVSQTEEKLLQKPCKELFSACVQSVHDYLRGEPFHEYLDSMYFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSRFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHHENIVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVPIPWQSEMIETECFKELNVFGPHGTLSPDLNRS
HPPEPPKKGLLQRLFKRQHQNNSKSSPNSKTSFNHHINSNHVSSNSTGSS
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BDBM50260130 |
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n/a |
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Name | BDBM50260130 |
Synonyms: | CHEMBL4090923 |
Type | Small organic molecule |
Emp. Form. | C29H31FN2O6 |
Mol. Mass. | 522.5646 |
SMILES | COc1cccc(OC)c1CNC(=O)c1cc(ccc1F)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1 |r| |
Structure |
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