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Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe.
Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Weaver CD, et al. Among authors: williams r. Curr Top Med Chem. 2009;9(13):1217-26. doi: 10.2174/156802609789753635. Curr Top Med Chem. 2009. PMID: 19807667 Free PMC article. Review.
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Lewis LM, et al. Among authors: williams l, williams r. Bioorg Med Chem Lett. 2008 Feb 1;18(3):885-90. doi: 10.1016/j.bmcl.2007.12.051. Epub 2008 Jan 4. Bioorg Med Chem Lett. 2008. PMID: 18178088 Free PMC article.
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Marlo JE, et al. Among authors: williams mb, williams r. Mol Pharmacol. 2009 Mar;75(3):577-88. doi: 10.1124/mol.108.052886. Epub 2008 Dec 1. Mol Pharmacol. 2009. PMID: 19047481 Free PMC article.
A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. Sheffler DJ, et al. Among authors: williams r. Mol Pharmacol. 2009 Aug;76(2):356-68. doi: 10.1124/mol.109.056531. Epub 2009 Apr 30. Mol Pharmacol. 2009. PMID: 19407080 Free PMC article.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Engers DW, et al. Among authors: williams r. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. Epub 2010 Jul 8. Bioorg Med Chem Lett. 2010. PMID: 20667732 Free PMC article.
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.
Sheffler DJ, Nedelcovych MT, Williams R, Turner SC, Duerk BB, Robbins MR, Jadhav SB, Niswender CM, Jones CK, Conn PJ, Daniels RN, Lindsley CW. Sheffler DJ, et al. Among authors: williams r. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1062-6. doi: 10.1016/j.bmcl.2014.01.011. Epub 2014 Jan 13. Bioorg Med Chem Lett. 2014. PMID: 24462664 Free PMC article.
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