Reaction Details |
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Target | G protein-coupled receptor kinase 5 |
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Ligand | BDBM283998 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1771207 (CHEMBL4223319) |
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IC50 | 260±n/a nM |
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Citation | Waldschmidt, HV; Bouley, R; Kirchhoff, PD; Lee, P; Tesmer, JJG; Larsen, SD Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg Med Chem Lett28:1507-1515 (2018) [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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BDBM283998 |
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n/a |
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Name | BDBM283998 |
Synonyms: | E24 | US10023564, Example 24 |
Type | Small organic molecule |
Emp. Form. | C25H23FN8O5 |
Mol. Mass. | 534.4991 |
SMILES | COCc1noc(CNC(=O)c2cc(ccc2F)C2NC(=O)NC(C)=C2C(=O)Nc2ccc3[nH]ncc3c2)n1 |c:25| |
Structure |
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