Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 11, 2010, Pages 3436-3440

  Harris III, Ralph N ^a   Stabler, Russel S ^a   Repke, David B ^a   Kress, James M ^a   Walker, Keith A ^a   Martin, Renee S ^a   Brothers, Julie M ^a   Ilnicka, Mariola ^a   Lee, Simon W ^a   Mirzadegan, Tara ^a  

^a ROCHE BIOSCIENCE   (United States)

Author keywords

1,6 Disubstituted tetralins; 5 HT6 neutal antagonist; Binding model; Non basic ligands; Receptor point mutation

Indexed keywords

SEROTONIN 6 ANTAGONIST;

ARTICLE; DRUG BINDING; DRUG POTENCY; DRUG STRUCTURE; MOLECULAR MODEL; POINT MUTATION; STRUCTURE ACTIVITY RELATION;

LIGANDS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; RECEPTORS, SEROTONIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77953288362     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.110     Document Type: Article

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