Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.

Tellew, John E; Lanier, Marion; Moorjani, Manisha; Lin, Emily; Luo, Zhiyong; Slee, Deborah H; Zhang, Xiaohu; Hoare, Sam R J; Grigoriadis, Dimitri E; St Denis, Yves; Di Fabio, Romano; Di Modugno, Enza; Saunders, John; Williams, John P

Tellew, John E; Lanier, Marion; Moorjani, Manisha; Lin, Emily; Luo, Zhiyong; Slee, Deborah H; Zhang, Xiaohu; Hoare, Sam R J; Grigoriadis, Dimitri E; St Denis, Yves; Di Fabio, Romano; Di Modugno, Enza; Saunders, John; Williams, John P.

Affiliation

Tellew JE; Department of Medicinal Chemistry, Neurocrine Biosciences, San Diego, CA 92130, USA.

Bioorg Med Chem Lett ; 20(24): 7259-64, 2010 Dec 15.

Article in En | MEDLINE | ID: mdl-21074436

Subject(s)

Azabicyclo Compounds/chemistry; Oxadiazoles/chemistry; Pyrazoles/chemistry; Pyridines/chemistry; Receptors, Corticotropin-Releasing Hormone/antagonists & inhibitors; Azabicyclo Compounds/chemical synthesis; Azabicyclo Compounds/pharmacokinetics; Humans; Microsomes, Liver/metabolism; Oxadiazoles/chemical synthesis; Oxadiazoles/pharmacokinetics; Protein Binding; Receptors, Corticotropin-Releasing Hormone/genetics; Receptors, Corticotropin-Releasing Hormone/metabolism; Recombinant Proteins/antagonists & inhibitors; Recombinant Proteins/genetics; Recombinant Proteins/metabolism

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oxadiazoles / Pyrazoles / Pyridines / Receptors, Corticotropin-Releasing Hormone / Azabicyclo Compounds Type of study: Prognostic_studies Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United States Country of publication: United kingdom

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