Document Report Card

ID: ALA1138060

Journal: J Med Chem

Title: 3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists.

Authors: Konkel MJ, Lagu B, Boteju LW, Jimenez H, Noble S, Walker MW, Chandrasena G, Blackburn TP, Nikam SS, Wright JL, Kornberg BE, Gregory T, Pugsley TA, Akunne H, Zoski K, Wise LD.

Abstract: A series of 3-imino-2-indolones are the first published, high-affinity antagonists of the galanin GAL3 receptor. One example, 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (9), was shown to have high affinity for the human GAL3 receptor (Ki=17 nM) and to be highly selective for GAL3 over a broad panel of targets, including GAL1 and GAL2. Compound 9 was also shown to be an antagonist in a human GAL3 receptor functional assay (Kb=29 nM).

CiteXplore: 16789730

DOI: 10.1021/jm060001n