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Identification of a Potent Agonist of the Orphan Nuclear Receptor Nurr1
Author(s) -
Dubois Celine,
Hengerer Bastian,
Mattes Henri
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600078
Subject(s) - agonist , nuclear receptor , orphan receptor , computational biology , benzimidazole , chemistry , identification (biology) , computer science , receptor , pharmacology , combinatorial chemistry , stereochemistry , bioinformatics , biology , biochemistry , gene , botany , transcription factor , organic chemistry
Benzimidazole‐based Nurr1 agonists : Combinatorial chemistry and structure‐based design were joined together to produce a lead‐finding library of compounds focused on the nuclear receptor target family. A second‐generation library directed against Nurr1, a specific orphan member of this family, was also prepared. This protocol allowed the discovery of a Nurr1 agonist with an EC 50 value of 8 n M .
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