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

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).

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

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

doi

10.1021/jm060001n

subject

Has Abstract

pub_date

2006-06-29 00:00:00

pages

3757-8

issue

13

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

杂志文章

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