(S)-VU0637120 is a Y4R antagonist that effectively reduces the binding response of its endogenous ligand, pancreatic polypeptide (PP), on Y4R, with an IC50 value of 2.7 μM. (S)-VU0637120 binds to the allosteric site of Y4R, which is located in the core region of the Y4R transmembrane structure, near the binding pocket of pancreatic polypeptide (PP), with a K B value of 300-400 nM. (S)-VU0637120 holds potential for research in the field of metabolic diseases [1].
References:
[1]. Schüß C, et al. Highly Selective Y Receptor Antagonist Binds in an Allosteric Binding Pocket. J Med Chem. 2021 Mar 11;64(5):2801-2814.
References:
[1]. Schüß C, et al. Highly Selective Y Receptor Antagonist Binds in an Allosteric Binding Pocket. J Med Chem. 2021 Mar 11;64(5):2801-2814.