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Chen HY, Plummer CW, Xiao D, et al. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS Med Chem Lett. 2018;9(7):685-690doi: 10.1021/acsmedchemlett.8b00149.
Chen, H. Y., Plummer, C. W., Xiao, D., Chobanian, H. R., DeMong, D., Miller, M., Trujillo, M. E., Kirkland, M., Kosinski, D., Mane, J., Pachanski, M., Cheewatrakoolpong, B., Di Salvo, J., Thomas-Fowlkes, B., Souza, S., Tatosian, D. A., Chen, Q., Hafey, M. J., Houle, R., Nolting, A. F., Orr, R., Ehrhart, J., Weinglass, A. B., Tschirret-Guth, R., Howard, A. D., & Colletti, S. L. (2018). Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS medicinal chemistry letters, 9(7), 685-690. https://doi.org/10.1021/acsmedchemlett.8b00149
Chen, Helen Y, et al. "Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs." ACS medicinal chemistry letters vol. 9,7 (2018): 685-690. doi: https://doi.org/10.1021/acsmedchemlett.8b00149
Chen HY, Plummer CW, Xiao D, Chobanian HR, DeMong D, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Di Salvo J, Thomas-Fowlkes B, Souza S, Tatosian DA, Chen Q, Hafey MJ, Houle R, Nolting AF, Orr R, Ehrhart J, Weinglass AB, Tschirret-Guth R, Howard AD, Colletti SL. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. doi: 10.1021/acsmedchemlett.8b00149. eCollection 2018 Jul 12. PMID: 30034601; PMCID: PMC6047031.
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ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. doi: 10.1021/acsmedchemlett.8b00149. eCollection 2018 Jul 12.

Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.

ACS medicinal chemistry letters

Helen Y Chen, Christopher W Plummer, Dong Xiao, Harry R Chobanian, Duane DeMong, Michael Miller, Maria E Trujillo, Melissa Kirkland, Daniel Kosinski, Joel Mane, Michele Pachanski, Boonlert Cheewatrakoolpong, Jerry Di Salvo, Brande Thomas-Fowlkes, Sarah Souza, Daniel A Tatosian, Qing Chen, Michael J Hafey, Robert Houle, Andrew F Nolting, Robert Orr, Juliann Ehrhart, Adam B Weinglass, Richard Tschirret-Guth, Andrew D Howard, Steven L Colletti

Affiliations

  1. Departments of Discovery Chemistry, Process Chemistry, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, In Vivo Pharmacology, and In Vitro Pharmacology, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

PMID: 30034601 PMCID: PMC6047031 DOI: 10.1021/acsmedchemlett.8b00149

Abstract

A series of biaryl chromans exhibiting potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM) were discovered as potential therapeutics for the treatment of type II diabetes. Optimization of physicochemical properties through modification of the pendant aryl rings resulted in the identification of compound

Conflict of interest statement

The authors declare no competing financial interest.

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