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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).
Reed CW, Yohn SE, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Reed CW, et al. Among authors: jenkins mt. J Med Chem. 2019 Feb 14;62(3):1690-1695. doi: 10.1021/acs.jmedchem.8b01810. Epub 2019 Jan 17. J Med Chem. 2019. PMID: 30608678 Free PMC article.
Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Temple KJ, et al. Among authors: jenkins mt. Bioorg Med Chem Lett. 2019 Nov 1;29(21):126678. doi: 10.1016/j.bmcl.2019.126678. Epub 2019 Sep 10. Bioorg Med Chem Lett. 2019. PMID: 31537424
Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.
Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Kalbfleisch JJ, et al. Among authors: jenkins mt. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127529. doi: 10.1016/j.bmcl.2020.127529. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890686 Free PMC article.
The delta isoform of phosphatidylinositol-3-kinase predominates in chronic myelomonocytic leukemia and can be targeted effectively with umbralisib and ruxolitinib.
Villaume MT, Arrate MP, Ramsey HE, Sunthankar KI, Jenkins MT, Moyo TK, Smith BN, Fischer MA, Childress MA, Gorska AE, Ferrell PB, Savona MR. Villaume MT, et al. Among authors: jenkins mt. Exp Hematol. 2021 May;97:57-65.e5. doi: 10.1016/j.exphem.2021.02.008. Epub 2021 Feb 19. Exp Hematol. 2021. PMID: 33617893 Free PMC article.
Multiomic profiling of human clonal hematopoiesis reveals genotype and cell-specific inflammatory pathway activation.
Heimlich JB, Bhat P, Parker AC, Jenkins MT, Vlasschaert C, Ulloa J, Van Amburg JC, Potts CR, Olson S, Silver AJ, Ahmad A, Sharber B, Brown D, Hu N, van Galen P, Savona MR, Bick AG, Ferrell PB. Heimlich JB, et al. Among authors: jenkins mt. Blood Adv. 2024 Jul 23;8(14):3665-3678. doi: 10.1182/bloodadvances.2023011445. Blood Adv. 2024. PMID: 38507736 Free PMC article.
63 results