SUFUGOLIX
Title | Journal |
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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 20110728 |
Non-peptide gonadotropin-releasing hormone receptor antagonists. | Journal of medicinal chemistry 20080626 |
Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor. | Molecular pharmacology 20080601 |
Trapping of a nonpeptide ligand by the extracellular domains of the gonadotropin-releasing hormone receptor results in insurmountable antagonism. | Molecular pharmacology 20070801 |
Challenges and opportunities of trapping ligands. | Molecular pharmacology 20070801 |
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 of medicinal chemistry 20061019 |
[An outline of GnRH analogue]. | Nihon rinsho. Japanese journal of clinical medicine 20060401 |
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. | Journal of medicinal chemistry 20060126 |
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists. | Bioorganic & medicinal chemistry letters 20031020 |
Suppression of a pituitary-ovarian axis by chronic oral administration of a novel nonpeptide gonadotropin-releasing hormone antagonist, TAK-013, in cynomolgus monkeys. | The Journal of clinical endocrinology and metabolism 20030401 |
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 of medicinal chemistry 20030102 |