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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.
Davis DC, Bungard JD, Chang S, Rodriguez AL, Blobaum AL, Boutaud O, Melancon BJ, Niswender CM, Jeffrey Conn P, Lindsley CW. Davis DC, et al. Among authors: jeffrey conn p. Bioorg Med Chem Lett. 2021 Jan 15;32:127724. doi: 10.1016/j.bmcl.2020.127724. Epub 2020 Nov 27. Bioorg Med Chem Lett. 2021. PMID: 33253881
Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Jeffrey Conn P, Bridges TM, Lindsley CW. Tarr JC, et al. Among authors: jeffrey conn p. Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014. doi: 10.1016/j.bmcl.2018.07.022. Epub 2018 Jul 31. Bioorg Med Chem Lett. 2018. PMID: 30076050 Free PMC article. No abstract available.
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.
Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Spearing PK, et al. Among authors: jeffrey conn p. Bioorg Med Chem Lett. 2021 Sep 1;47:128193. doi: 10.1016/j.bmcl.2021.128193. Epub 2021 Jun 9. Bioorg Med Chem Lett. 2021. PMID: 34118412 Free PMC article.
Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.
Yamada Y, Gilliland K, Xiang Z, Haymer D, Crocker KE, Loch MT, Schulte ML, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Melancon BJ. Yamada Y, et al. Among authors: jeffrey conn p. Bioorg Med Chem Lett. 2021 Oct 15;50:128342. doi: 10.1016/j.bmcl.2021.128342. Epub 2021 Aug 27. Bioorg Med Chem Lett. 2021. PMID: 34461178