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BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Marcin LR, Warrier J, Thangathirupathy S, Shi J, Karageorge GN, Pearce BC, Ng A, Park H, Kempson J, Li J, Zhang H, Mathur A, Reddy AB, Nagaraju G, Tonukunuru G, Gupta GVRKM, Kamble M, Mannoori R, Cheruku S, Jogi S, Gulia J, Bastia T, Sanmathi C, Aher J, Kallem R, Srikumar BN, Vijaya KK, Naidu PS, Paschapur M, Kalidindi N, Vikramadithyan R, Ramarao M, Denton R, Molski T, Shields E, Subramanian M, Zhuo X, Nophsker M, Simmermacher J, Sinz M, Albright C, Bristow LJ, Islam I, Bronson JJ, Olson RE, King D, Thompson LA, Macor JE. Marcin LR, et al. Among authors: park h. ACS Med Chem Lett. 2018 Apr 13;9(5):472-477. doi: 10.1021/acsmedchemlett.8b00080. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795762 Free PMC article.
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents.
Wu YJ, Guernon J, Yang F, Snyder L, Shi J, Mcclure A, Rajamani R, Park H, Ng A, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA. Wu YJ, et al. Among authors: park h. ACS Med Chem Lett. 2016 Jan 11;7(3):271-6. doi: 10.1021/acsmedchemlett.5b00432. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985314 Free PMC article.
Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor.
Cook J, Zusi FC, Hill MD, Fang H, Pearce B, Park H, Gallagher L, McDonald IM, Bristow L, Macor JE, Olson RE. Cook J, et al. Among authors: park h. Bioorg Med Chem Lett. 2017 Nov 15;27(22):5002-5005. doi: 10.1016/j.bmcl.2017.10.009. Epub 2017 Oct 10. Bioorg Med Chem Lett. 2017. PMID: 29050783
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM. Sivaprakasam P, et al. Among authors: park h. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25845281
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Regueiro-Ren A, Sit SY, Chen Y, Chen J, Swidorski JJ, Liu Z, Venables BL, Sin N, Hartz RA, Protack T, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Gupta A, Rampulla R, Mathur A, Park H, Sarjeant A, Benitex Y, Rahematpura S, Parker D, Phillips T, Haskell R, Jenkins S, Santone KS, Cockett M, Hanumegowda U, Dicker I, Meanwell NA, Krystal M. Regueiro-Ren A, et al. Among authors: park h. J Med Chem. 2022 Sep 22;65(18):11927-11948. doi: 10.1021/acs.jmedchem.2c00879. Epub 2022 Aug 31. J Med Chem. 2022. PMID: 36044257
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
Wurtz NR, Johnson JA, Viet A, Shirude PS, Baligar V, Madduri S, Cheney DL, Park H, Lupisella JA, Hsu MY, Abousleiman M, Galella MA, Aulakh D, Dierks EA, Garcia RA, Ostrowski J, Kick EK, Wexler RR. Wurtz NR, et al. Among authors: park h. ACS Med Chem Lett. 2022 May 25;13(6):943-948. doi: 10.1021/acsmedchemlett.2c00079. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707160 Free PMC article.
Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.
Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS. Liu C, et al. Among authors: park h. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891145 Free PMC article.
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists.
Marcoux D, Bertrand MB, Weigelt CA, Yip S, Galella M, Park H, Wu DR, Wang J, Yarde M, Cvijic ME, Li S, Hynes J Jr, Tino JA, Zhao Q, Dhar TGM. Marcoux D, et al. Among authors: park h. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127466. doi: 10.1016/j.bmcl.2020.127466. Epub 2020 Aug 5. Bioorg Med Chem Lett. 2020. PMID: 32763309
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