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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. 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 VU6007496: Challenges in the Development of an M1 Positive Allosteric Modulator Backup Candidate.
Engers JL, Bollinger KA, Capstick RA, Long MF, Bender AM, Dickerson JW, Peng W, Presley CC, Cho HP, Rodriguez AL, Niswender CM, Moran SP, Xiang Z, Blobaum AL, Boutaud O, Rook JM, Engers DW, Conn PJ, Lindsley CW. Engers JL, et al. ACS Chem Neurosci. 2024 Sep 18;15(18):3421-3433. doi: 10.1021/acschemneuro.4c00508. Epub 2024 Aug 28. ACS Chem Neurosci. 2024. PMID: 39197083 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: engers jl. 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.
Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor.
Li J, Orsi DL, Engers JL, Long MF, Capstick RA, Maurer MA, Presley CC, Vinson PN, Rodriguez AL, Han A, Cho HP, Chang S, Jackson M, Bubser M, Blobaum AL, Boutaud O, Nader MA, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Li J, et al. Among authors: engers jl. J Med Chem. 2024 Aug 22;67(16):14394-14413. doi: 10.1021/acs.jmedchem.4c01193. Epub 2024 Aug 6. J Med Chem. 2024. PMID: 39105778 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: engers jl. 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 the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.
Moehle MS, Bender AM, Dickerson JW, Foster DJ, Qi A, Cho HP, Donsante Y, Peng W, Bryant Z, Stillwell KJ, Bridges TM, Chang S, Watson KJ, O'Neill JC, Engers JL, Peng L, Rodriguez AL, Niswender CM, Lindsley CW, Hess EJ, Conn PJ, Rook JM. Moehle MS, et al. Among authors: engers jl. ACS Pharmacol Transl Sci. 2021 Aug 2;4(4):1306-1321. doi: 10.1021/acsptsci.0c00162. eCollection 2021 Aug 13. ACS Pharmacol Transl Sci. 2021. PMID: 34423268 Free PMC article.
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.
Spock M, Carter TR, Bollinger KA, Han C, Baker LA, Rodriguez AL, Peng L, Dickerson JW, Qi A, Rook JM, O'Neill JC, Watson KJ, Chang S, Bridges TM, Engers JL, Engers DW, Niswender CM, Conn PJ, Lindsley CW, Bender AM. Spock M, et al. Among authors: engers jl. ACS Med Chem Lett. 2021 Aug 2;12(8):1342-1349. doi: 10.1021/acsmedchemlett.1c00363. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413964 Free PMC article.
39 results