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Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM).
Engers JL, Baker LA, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Cho HP, Bubser M, Gray AT, Jones CK, Peng W, Rook JM, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ. Engers JL, et al. Among authors: luscombe vb. ACS Chem Neurosci. 2024 Sep 24;15(20):3744-54. doi: 10.1021/acschemneuro.4c00465. Online ahead of print. ACS Chem Neurosci. 2024. PMID: 39316465 Free PMC article.
Discovery of VU6008677: A Structurally Distinct Tricyclic M4 Positive Allosteric Modulator with Improved CYP450 Profile.
Capstick RA, Bollinger SR, Engers JL, Long MF, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ. Capstick RA, et al. Among authors: luscombe vb. ACS Med Chem Lett. 2024 Jul 3;15(8):1358-1366. doi: 10.1021/acsmedchemlett.4c00249. eCollection 2024 Aug 8. ACS Med Chem Lett. 2024. PMID: 39140069 Free PMC article.
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2.
Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Lindsley CW, Engers DW, Temple KJ. Long MF, et al. Among authors: luscombe vb. Bioorg Med Chem Lett. 2021 Dec 1;53:128416. doi: 10.1016/j.bmcl.2021.128416. Epub 2021 Oct 26. Bioorg Med Chem Lett. 2021. PMID: 34710625 Free PMC article.
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: luscombe vb. 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.
33 results