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549 results

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Page 1
Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.
Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J. Frankowski KJ, et al. Among authors: smith lh. ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. doi: 10.1021/cn200128x. Epub 2012 Jan 20. ACS Chem Neurosci. 2012. PMID: 22737280 Free PMC article.
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Li Y, Milewski M, Gosalia P, Gray W, Mehta A, Sugarman E, Hood B, Suyama E, Nguyen K, Heynen-Genel S, Vasile S, Salaniwal S, Stonich D, Su Y, Mangravita-Novo A, Vicchiarelli M, Roth GP, Smith LH, Chung TD, Hanson GR, Thomas JB, Caron MG, Barak LS, Pinkerton AB. Peddibhotla S, et al. Among authors: smith lh. ACS Med Chem Lett. 2013 Jul 20;4(9):846-851. doi: 10.1021/ml400176n. ACS Med Chem Lett. 2013. PMID: 24611085 Free PMC article.
Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response.
Flaherty DP, Miller JR, Garshott DM, Hedrick M, Gosalia P, Li Y, Milewski M, Sugarman E, Vasile S, Salaniwal S, Su Y, Smith LH, Chung TD, Pinkerton AB, Aubé J, Callaghan MU, Golden JE, Fribley AM, Kaufman RJ. Flaherty DP, et al. Among authors: smith lh. ACS Med Chem Lett. 2014 Oct 29;5(12):1278-1283. doi: 10.1021/ml5003234. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25530830 Free PMC article.
Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.
Peddibhotla S, Fontaine P, Leung CK, Maloney P, Hershberger PM, Wang Y, Bousquet MS, Luesch H, Mangravita-Novo A, Pinkerton AB, Smith LH, Malany S, Choe K. Peddibhotla S, et al. Among authors: smith lh. ACS Chem Biol. 2015 Aug 21;10(8):1871-9. doi: 10.1021/acschembio.5b00304. Epub 2015 May 22. ACS Chem Biol. 2015. PMID: 25946346
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Maloney PR, Khan P, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TD, Smith LH, Pinkerton AB. Maloney PR, et al. Among authors: smith lh. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60. doi: 10.1016/j.bmcl.2012.08.105. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010269 Free PMC article.
Imidazole-derived agonists for the neurotensin 1 receptor.
Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP. Hershberger PM, et al. Among authors: smith lh. Bioorg Med Chem Lett. 2014 Jan 1;24(1):262-7. doi: 10.1016/j.bmcl.2013.11.026. Epub 2013 Nov 21. Bioorg Med Chem Lett. 2014. PMID: 24332089 Free PMC article.
Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation.
Khan PM, Correa RG, Divlianska DB, Peddibhotla S, Sessions EH, Magnuson G, Brown B, Suyama E, Yuan H, Mangravita-Novo A, Vicchiarelli M, Su Y, Vasile S, Smith LH, Diaz PW, Reed JC, Roth GP. Khan PM, et al. Among authors: smith lh. ACS Med Chem Lett. 2011 Oct 13;2(10):780-785. doi: 10.1021/ml200158b. Epub 2011 Aug 5. ACS Med Chem Lett. 2011. PMID: 22003428 Free PMC article.
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, Hershberger P, Hedrick MP, Falter B, Ardecky RJ, Smith LH, Chung TDY, Jackson MR, Caron MG, Barak LS. Pinkerton AB, et al. Among authors: smith lh. J Med Chem. 2019 Sep 12;62(17):8357-8363. doi: 10.1021/acs.jmedchem.9b00340. Epub 2019 Aug 20. J Med Chem. 2019. PMID: 31390201 Free PMC article.
Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.
Dahl R, Bravo Y, Sharma V, Ichikawa M, Dhanya RP, Hedrick M, Brown B, Rascon J, Vicchiarelli M, Mangravita-Novo A, Yang L, Stonich D, Su Y, Smith LH, Sergienko E, Freeze HH, Cosford ND. Dahl R, et al. Among authors: smith lh. J Med Chem. 2011 May 26;54(10):3661-8. doi: 10.1021/jm101401a. Epub 2011 May 3. J Med Chem. 2011. PMID: 21539312 Free PMC article.
Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.
Preuss J, Maloney P, Peddibhotla S, Hedrick MP, Hershberger P, Gosalia P, Milewski M, Li YL, Sugarman E, Hood B, Suyama E, Nguyen K, Vasile S, Sergienko E, Mangravita-Novo A, Vicchiarelli M, McAnally D, Smith LH, Roth GP, Diwan J, Chung TD, Jortzik E, Rahlfs S, Becker K, Pinkerton AB, Bode L. Preuss J, et al. Among authors: smith lh. J Med Chem. 2012 Aug 23;55(16):7262-72. doi: 10.1021/jm300833h. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22813531 Free PMC article.
549 results