Discovery of Sodium <i>R</i>-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2<i>H</i>-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

Chen Chen, Dongpei Wu, Zhiqiang Guo, +16

Journal of Medicinal Chemistry

Novel Uracil PhenylethylaminesGynecologyPharmacotherapyExperimental PharmacologyMolecular Pharmacology +14

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX

John H. Hutchinson, Martin W. Rowbottom, David Lonergan, +5

ACS Medicinal Chemistry Letters

Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2)

Martin W. Rowbottom, Gretchen Bain, Imelda Calderon, +15

Journal of Medicinal Chemistry

Initial Hit 2PharmacotherapyChemical BiologyPharmaceutical ChemistryChemical Derivative +19

Potent imidazole and triazole CB 1 receptor antagonists related to SR141716

Brian Dyck, Val S. Goodfellow, Teresa A. Phillips, +6

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyBiochemistryFunctional SelectivityMedicineReceptor Antagonists +8

Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E

Martin W. Rowbottom, Raffaella Faraoni, Qi Chao, +29

Journal of Medicinal Chemistry

Orally Efficacious InhibitorChemoprevention StrategyImmunologySeveral BrafAntiviral Drug +17

3-[(2<i>R</i>)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a Potent and Orally Active Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Design, Synthesis, and in Vitro and in Vivo Characterization

Fábio C. Tucci, Yunfei Zhu, R. Scott Struthers, +14

Journal of Medicinal Chemistry

Pharmaceutical ScienceSubstituted UracilsPeptide SciencePharmacotherapyNbi 42902 +18

CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and <i>In Vivo</i> Antitumor Activity

Joyce James, Bruce Ruggeri, Robert C. Armstrong, +20

Molecular Cancer Therapeutics

Tumor BiologyActive Braf InhibitorNovel TherapyBraf GeneMedicine +13

Synthesis and Structure−Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists

Zhiqiang Guo, Yunfei Zhu, Timothy D. Gross, +13

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryMethyl GroupUracil CompoundsBiochemistry +13

A Thienopyridazinone-Based Melanin-Concentrating Hormone Receptor 1 Antagonist with Potent in Vivo Anorectic Properties

Brian Dyck, Stacy Markison, Liren Zhao, +14

Journal of Medicinal Chemistry

Medicinal ChemistryPharmacological StudyFunctional SelectivityMedicineHormone Receptor +12

3-(2-Aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl- uracils as Orally Bioavailable Antagonists of the Human Gonadotropin Releasing Hormone Receptor

Fábio C. Tucci, Yunfei Zhu, Zhiqiang Guo, +14

Journal of Medicinal Chemistry

Pharmaceutical SciencePotent Human GonadotropinPharmacotherapyHormone Receptor AntagonistsPharmaceutical Chemistry +17