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Page 1
A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors.
Bolduc PN, Pfaffenbach M, Evans R, Xin Z, Henry KL, Gao F, Fang T, Silbereis J, Vera Rebollar J, Li P, Chodaparambil JV, Metrick C, Peterson EA. Bolduc PN, et al. Among authors: chodaparambil jv. ACS Med Chem Lett. 2024 Apr 26;15(5):714-721. doi: 10.1021/acsmedchemlett.4c00102. eCollection 2024 May 9. ACS Med Chem Lett. 2024. PMID: 38746903
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
Evans R, Bolduc PN, Pfaffenbach M, Gao F, May-Dracka T, Fang T, Hopkins BT, Chodaparambil JV, Henry KL, Li P, Metrick C, Nelson A, Trapa P, Thomas A, Burkly L, Peterson EA. Evans R, et al. Among authors: chodaparambil jv. J Med Chem. 2024 Mar 28;67(6):4676-4690. doi: 10.1021/acs.jmedchem.3c02226. Epub 2024 Mar 11. J Med Chem. 2024. PMID: 38467640
Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
Pfaffenbach M, Bolduc PN, Xin Z, Gao F, Evans R, Fang T, Chodaparambil JV, Henry KL, Li P, Mathieu S, Metrick C, Vera Rebollar JA, Gu RF, Mccarl CA, Silbereis J, Peterson EA. Pfaffenbach M, et al. Among authors: chodaparambil jv. J Med Chem. 2024 May 23;67(10):8383-8395. doi: 10.1021/acs.jmedchem.4c00560. Epub 2024 May 2. J Med Chem. 2024. PMID: 38695469
Elucidation of the GSK3α Structure Informs the Design of Novel, Paralog-Selective Inhibitors.
Amaral B, Capacci A, Anderson T, Tezer C, Bajrami B, Lulla M, Lucas B, Chodaparambil JV, Marcotte D, Kumar PR, Murugan P, Spilker K, Cullivan M, Wang T, Peterson AC, Enyedy I, Ma B, Chen T, Yousaf Z, Calhoun M, Golonzhka O, Dillon GM, Koirala S. Amaral B, et al. Among authors: chodaparambil jv. ACS Chem Neurosci. 2023 Mar 15;14(6):1080-1094. doi: 10.1021/acschemneuro.2c00476. Epub 2023 Feb 22. ACS Chem Neurosci. 2023. PMID: 36812145 Free PMC article.
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
May-Dracka TL, Gao F, Hopkins BT, Hronowski X, Chen T, Chodaparambil JV, Metrick CM, Cullivan M, Enyedy I, Kaliszczak M, Kankel MW, Marx I, Michell-Robinson MA, Murugan P, Kumar PR, Rooney M, Schuman E, Sen A, Wang T, Ye T, Peterson EA. May-Dracka TL, et al. Among authors: chodaparambil jv. ACS Med Chem Lett. 2022 Mar 3;13(4):665-673. doi: 10.1021/acsmedchemlett.1c00682. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450377 Free PMC article.
Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.
Ma B, Zhang L, Sun L, Xin Z, Kumaravel G, Marcotte D, Chodaparambil JV, Wang Q, Wehr A, Jing J, Hong VS, Wang T, Huang C, Shao Z, Mi S. Ma B, et al. Among authors: chodaparambil jv. ACS Med Chem Lett. 2021 Jun 14;12(7):1124-1129. doi: 10.1021/acsmedchemlett.1c00211. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267882 Free PMC article.
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Halkina T, Henderson JL, Lin EY, Himmelbauer MK, Jones JH, Nevalainen M, Feng J, King K, Rooney M, Johnson JL, Marcotte DJ, Chodaparambil JV, Kumar PR, Patterson TA, Murugan P, Schuman E, Wong L, Hesson T, Lamore S, Bao C, Calhoun M, Certo H, Amaral B, Dillon GM, Gilfillan R, de Turiso FG. Halkina T, et al. Among authors: chodaparambil jv. J Med Chem. 2021 May 13;64(9):6358-6380. doi: 10.1021/acs.jmedchem.1c00382. Epub 2021 May 4. J Med Chem. 2021. PMID: 33944571
Human PLD structures enable drug design and characterization of isoenzyme selectivity.
Metrick CM, Peterson EA, Santoro JC, Enyedy IJ, Murugan P, Chen T, Michelsen K, Cullivan M, Spilker KA, Kumar PR, May-Dracka TL, Chodaparambil JV. Metrick CM, et al. Among authors: chodaparambil jv. Nat Chem Biol. 2020 Apr;16(4):391-399. doi: 10.1038/s41589-019-0458-4. Epub 2020 Feb 10. Nat Chem Biol. 2020. PMID: 32042197
21 results