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26 results

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Page 1
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.
Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Tarr JC, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995. doi: 10.1016/j.bmcl.2017.05.014. Epub 2017 May 6. Bioorg Med Chem Lett. 2017. PMID: 28522253 Free PMC article.
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.
Lebois EP, Digby GJ, Sheffler DJ, Melancon BJ, Tarr JC, Cho HP, Miller NR, Morrison R, Bridges TM, Xiang Z, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Lebois EP, et al. Among authors: tarr jc. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6451-5. doi: 10.1016/j.bmcl.2011.08.084. Epub 2011 Aug 24. Bioorg Med Chem Lett. 2011. PMID: 21930376 Free PMC article.
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: tarr jc. Bioorg Med Chem Lett. 2012 May 15;22(10):3467-72. doi: 10.1016/j.bmcl.2012.03.088. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22507963 Free PMC article.
Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.
Tarr JC, Turlington ML, Reid PR, Utley TJ, Sheffler DJ, Cho HP, Klar R, Pancani T, Klein MT, Bridges TM, Morrison RD, Blobaum AL, Xiang Z, Daniels JS, Niswender CM, Conn PJ, Wood MR, Lindsley CW. Tarr JC, et al. ACS Chem Neurosci. 2012 Nov 21;3(11):884-95. doi: 10.1021/cn300068s. Epub 2012 Jul 18. ACS Chem Neurosci. 2012. PMID: 23173069 Free PMC article.
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW. Sheffler DJ, et al. Among authors: tarr jc. Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7. doi: 10.1016/j.bmcl.2012.10.132. Epub 2012 Nov 9. Bioorg Med Chem Lett. 2013. PMID: 23200253 Free PMC article.
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.
Melancon BJ, Poslusney MS, Gentry PR, Tarr JC, Sheffler DJ, Mattmann ME, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: tarr jc. Bioorg Med Chem Lett. 2013 Jan 15;23(2):412-6. doi: 10.1016/j.bmcl.2012.11.092. Epub 2012 Dec 1. Bioorg Med Chem Lett. 2013. PMID: 23237839 Free PMC article.
Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100.
Byun NE, Grannan M, Bubser M, Barry RL, Thompson A, Rosanelli J, Gowrishankar R, Kelm ND, Damon S, Bridges TM, Melancon BJ, Tarr JC, Brogan JT, Avison MJ, Deutch AY, Wess J, Wood MR, Lindsley CW, Gore JC, Conn PJ, Jones CK. Byun NE, et al. Among authors: tarr jc. Neuropsychopharmacology. 2014 Jun;39(7):1578-93. doi: 10.1038/npp.2014.2. Epub 2014 Jan 20. Neuropsychopharmacology. 2014. PMID: 24442096 Free PMC article.
Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK. Bubser M, et al. Among authors: tarr jc. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19. ACS Chem Neurosci. 2014. PMID: 25137629 Free PMC article.
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Pelz NF, Bian Z, Zhao B, Shaw S, Tarr JC, Belmar J, Gregg C, Camper DV, Goodwin CM, Arnold AL, Sensintaffar JL, Friberg A, Rossanese OW, Lee T, Olejniczak ET, Fesik SW. Pelz NF, et al. Among authors: tarr jc. J Med Chem. 2016 Mar 10;59(5):2054-66. doi: 10.1021/acs.jmedchem.5b01660. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878343 Free PMC article.
26 results