Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Journal of medicinal chemistry • Vol. 54, Issue 14 • 2011
Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Molecular pharmacology • Vol. 73, Issue 6 • 2008
Trapping of a nonpeptide ligand by the extracellular domains of the gonadotropin-releasing hormone receptor results in insurmountable antagonism.
Molecular pharmacology • Vol. 72, Issue 2 • 2007
[An outline of GnRH analogue].
Nihon rinsho. Japanese journal of clinical medicine • Vol. 64 Suppl 4 • 2006
