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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: capstick ra. 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.
VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events.
Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW. Engers JL, et al. Among authors: capstick ra. ACS Med Chem Lett. 2018 Sep 4;9(9):917-922. doi: 10.1021/acsmedchemlett.8b00261. eCollection 2018 Sep 13. ACS Med Chem Lett. 2018. PMID: 30258541 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: capstick ra. 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.
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.
Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, Bubser M, Chang S, Schnetz-Boutaud NC, Boutaud O, Blobaum AL, Foster DJ, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Han C. Garrison AT, et al. Among authors: capstick ra. J Med Chem. 2022 Apr 28;65(8):6273-6286. doi: 10.1021/acs.jmedchem.2c00192. Epub 2022 Apr 13. J Med Chem. 2022. PMID: 35417155
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: capstick ra. 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. 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: capstick ra. 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.
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.
Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW. Panarese JD, et al. Among authors: capstick ra. Bioorg Med Chem Lett. 2019 Jan 15;29(2):342-346. doi: 10.1016/j.bmcl.2018.10.050. Epub 2018 Nov 1. Bioorg Med Chem Lett. 2019. PMID: 30503632