Discovery of a Biaryl Cyclohexene Carboxylic Acid (MK-6892): A Potent and Selective High Affinity Niacin Receptor Full Agonist with Reduced Flushing Profiles in Animals as a Preclinical Candidate

Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.

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PID https://www.doi.org/10.1021/jm100022r.s001
PID pmid:20184326
PID https://www.doi.org/10.1021/jm100022r
URL https://pubs.acs.org/doi/abs/10.1021/jm100022r
URL https://dx.doi.org/10.1021/jm100022r
URL https://core.ac.uk/display/152991202
URL http://dx.doi.org/10.1021/jm100022r
URL https://figshare.com/articles/journal_contribution/Discovery_of_a_Biaryl_Cyclohexene_Carboxylic_Acid_MK_6892_A_Potent_and_Selective_High_Affinity_Niacin_Receptor_Full_Agonist_with_Reduced_Flushing_Profiles_in_Animals_as_a_Preclinical_Candidate/2781763
URL https://academic.microsoft.com/#/detail/2024929585
URL https://pubs.acs.org/doi/pdf/10.1021/jm100022r
URL https://www.ncbi.nlm.nih.gov/pubmed/20184326
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Access Right Open Access
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Author Hong C. Shen
Author Fa-Xiang Ding
Author Subharekha Raghavan
Author Qiaolin Deng
Author Silvi Luell
Author Michael J. Forrest
Author Ester Carballo-Jane
Author Larissa C. Wilsie
Author Mihajlo L. Krsmanovic
Author Andrew K. Taggart
Author Kenneth K. Wu
Author Tsuei-Ju Wu
Author Kang Cheng
Author Ning Ren
Author Tian-Quan Cai
Author Qing Chen
Author Junying Wang
Author Michael S. Wolff
Author Xinchun Tong
Author Tom G. Holt
Author M. Gerard Waters
Author Milton L. Hammond
Author James R. Tata
Author Steven L. Colletti
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Collected From Europe PubMed Central; figshare; Datacite; Crossref; Microsoft Academic Graph
Hosted By figshare; Journal of Medicinal Chemistry
Publication Date 2010-03-25
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Language English
Resource Type Other literature type; Article; UNKNOWN
system:type publication
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Source https://science-innovation-policy.openaire.eu/search/publication?articleId=dedup_wf_001::36799af3bdd4faf514986bd1f77058ed
Author jsonws_user
Last Updated 23 December 2020, 01:34 (CET)
Created 23 December 2020, 01:34 (CET)