Reaction Details |
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Target | G protein-coupled receptor kinase 5 |
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Ligand | BDBM50529469 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1908743 (CHEMBL4411101) |
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IC50 | 350±n/a nM |
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Citation | Rowlands, RA; Cato, MC; Waldschmidt, HV; Bouley, RA; Chen, Q; Avramova, L; Larsen, SD; Tesmer, JJG; White, AD Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett10:1628-1634 (2019) [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 GRK5 | GPRK5 | GRK5 | GRK5_HUMAN |
Type: | PROTEIN |
Mol. Mass.: | 67798.93 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1280627 |
Residue: | 590 |
Sequence: | MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQ
PIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQ
VGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRN
HPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
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BDBM50529469 |
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n/a |
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Name | BDBM50529469 |
Synonyms: | CHEMBL4456539 |
Type | Small organic molecule |
Emp. Form. | C26H28N8O3 |
Mol. Mass. | 500.5523 |
SMILES | COc1cc(NC(=O)\C=C\CN(C)C)ccc1Nc1nc(Nc2ccccc2C(N)=O)c2cc[nH]c2n1 |
Structure |
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