| Reaction Details |
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 | Report a problem with these data |
| Target | G protein-coupled receptor kinase 5 |
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| Ligand | BDBM50173311 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1581285 (CHEMBL3811362) |
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| IC50 | 8100±n/a nM |
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| Citation |  Waldschmidt, HV; Homan, KT; Cruz-Rodríguez, O; Cato, MC; Waninger-Saroni, J; Larimore, KM; Cannavo, A; Song, J; Cheung, JY; Kirchhoff, PD; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem59:3793-807 (2016) [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 |
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| Synonyms: | G protein-coupled receptor kinase GRK5 | GPRK5 | GRK5 | GRK5_HUMAN |
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| Type: | PROTEIN |
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| Mol. Mass.: | 67798.93 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_1280627 |
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| Residue: | 590 |
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| Sequence: | MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQ
PIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQ
VGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRN
HPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
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| BDBM50173311 |
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| n/a |
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| Name | BDBM50173311 |
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| Synonyms: | CHEMBL3810073 | US10023564, Example 6 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H25FN6O4 |
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| Mol. Mass. | 528.5343 |
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| SMILES | COc1ccc(CNC(=O)c2cc(ccc2F)C2NC(=O)NC(C)=C2C(=O)Nc2ccc3[nH]ncc3c2)cc1 |c:24| |
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| Structure | 
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