Reaction Details |
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Target | G protein-coupled receptor kinase 5 |
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Ligand | BDBM22416 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1692746 |
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IC50 | >100000±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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BDBM22416 |
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n/a |
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Name | BDBM22416 |
Synonyms: | (3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | (3S,4R)-3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | CHEMBL490 | PAROXETINE | US09969700, Paroxetine | US9944618, Compound ID No. 182 | [3H]Paroxetine |
Type | radiolabeled ligand |
Emp. Form. | C19H20FNO3 |
Mol. Mass. | 329.3654 |
SMILES | Fc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1 |
Structure |
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