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Page 1
Discovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.
Childress ES, Capstick RA, Crocker KE, Ledyard ML, Bender AM, Maurer MA, Billard NB, Cho HP, Rodriguez AL, Niswender CM, Peng W, Rook JM, Chang S, Blobaum AL, Boutaud O, Thompson Gray A, Jones CK, Conn PJ, Felts AS, Lindsley CW, Temple KJ. Childress ES, et al. Among authors: boutaud o. ACS Med Chem Lett. 2024 Nov 18;15(12):2210-2219. doi: 10.1021/acsmedchemlett.4c00481. eCollection 2024 Dec 12. ACS Med Chem Lett. 2024. PMID: 39691522 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: boutaud o. 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 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: boutaud o. 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 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. Among authors: boutaud o. 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 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: boutaud o. 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 VU6024578/BI02982816: An mGlu1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models.
Reed CW, Kalbfleisch JF, Turkett JA, Trombley TA, Nastase AF, Spearing PK, Haymer DH, Sarwar MM, Quitalig M, Dickerson JW, Blobaum AL, Boutaud O, Voehringer P, Schuelert N, Cho HP, Niswender CM, Rook JM, Priepke H, Ursu D, Conn PJ, Melancon BJ, Lindsley CW. Reed CW, et al. Among authors: boutaud o. J Med Chem. 2024 Dec 26;67(24):22291-22312. doi: 10.1021/acs.jmedchem.4c02554. Epub 2024 Dec 12. J Med Chem. 2024. PMID: 39665415
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.
Dodd CJ, Chronister KS, Rathnayake U, Parr LC, Li K, Chang S, Mi D, Days EL, Bauer JA, Cho HP, Boutaud O, Denton JS, Lindsley CW, Han C. Dodd CJ, et al. Among authors: boutaud o. Bioorg Med Chem Lett. 2023 May 1;87:129256. doi: 10.1016/j.bmcl.2023.129256. Epub 2023 Mar 24. Bioorg Med Chem Lett. 2023. PMID: 36966977 Free PMC article.
Discovery of "Molecular Switches" within a Series of mGlu5 Allosteric Ligands Driven by a "Magic Methyl" Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype.
Barbaro L, Rodriguez AL, Blevins AN, Dickerson JW, Billard N, Boutaud O, Rook JL, Niswender CM, Conn PJ, Engers DW, Lindsley CW. Barbaro L, et al. Among authors: boutaud o. ACS Bio Med Chem Au. 2021 Aug 20;1(1):21-30. doi: 10.1021/acsbiomedchemau.1c00024. eCollection 2021 Dec 15. ACS Bio Med Chem Au. 2021. PMID: 37101980 Free PMC article.
96 results