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Updated: Aug 24, 2026

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N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists
Valentina Molteni1, Julie Penzotti, Dean M Wilson
1Bristol-Myers Squibb Pharma Research Laboratories, 4570 Executive Drive, Suite 400, San Diego, California 92121, USA.
Abstract:
Screening of a computationally designed synthetic library led to the discovery of the N-phenylphenylglycines (NPPGs) as a novel class of human corticotropin releasing factor (h-CRF(1)) antagonists. Several NPPGs with greater potency than the original hit 1 were rapidly identified, and resolution of the racemate demonstrated that only the R-enantiomer displays activity. This structural class represents the first example of a non-peptide CRF(1) antagonist with a stereochemically distinct receptor binding affinity.
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