Title: 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: Journal of medicinal chemistry20110728
Title: Non-peptide gonadotropin-releasing hormone receptor antagonists.
Journal: Journal of medicinal chemistry20080626
Title: Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Journal: Molecular pharmacology20080601
Title: Trapping of a nonpeptide ligand by the extracellular domains of the gonadotropin-releasing hormone receptor results in insurmountable antagonism.
Journal: Molecular pharmacology20070801
Title: Challenges and opportunities of trapping ligands.
Journal: Molecular pharmacology20070801
Title: Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.
Journal: Journal of medicinal chemistry20061019
Title: [An outline of GnRH analogue].
Journal: Nihon rinsho. Japanese journal of clinical medicine20060401
Title: Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
Journal: Journal of medicinal chemistry20060126
Title: Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Journal: Bioorganic & medicinal chemistry letters20031020
Title: Suppression of a pituitary-ovarian axis by chronic oral administration of a novel nonpeptide gonadotropin-releasing hormone antagonist, TAK-013, in cynomolgus monkeys.
Journal: The Journal of clinical endocrinology and metabolism20030401
Title: Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
Journal: Journal of medicinal chemistry20030102
Title: Sasaki S, et al. Discovery of a thieno,3-dpyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J Med Chem. 2003 Jan 2;46(1):113-24.
