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Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.
Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: kramer a. Molecules. 2024 Sep 2;29(17):4158. doi: 10.3390/molecules29174158. Molecules. 2024. PMID: 39275006 Free PMC article.
Development of a potent and selective chemical probe for the pleiotropic kinase CK2.
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD. Wells CI, et al. Among authors: kramer a. Cell Chem Biol. 2021 Apr 15;28(4):546-558.e10. doi: 10.1016/j.chembiol.2020.12.013. Epub 2021 Jan 22. Cell Chem Biol. 2021. PMID: 33484635 Free PMC article.
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH. Ong HW, et al. Among authors: kramer a. Eur J Med Chem. 2023 Mar 5;249:115043. doi: 10.1016/j.ejmech.2022.115043. Epub 2022 Dec 30. Eur J Med Chem. 2023. PMID: 36736152 Free PMC article.
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
Davis-Gilbert ZW, Krämer A, Dunford JE, Howell S, Senbabaoglu F, Wells CI, Bashore FM, Havener TM, Smith JL, Hossain MA, Oppermann U, Drewry DH, Axtman AD. Davis-Gilbert ZW, et al. Among authors: kramer a. ACS Med Chem Lett. 2023 Mar 14;14(4):432-441. doi: 10.1021/acsmedchemlett.2c00530. eCollection 2023 Apr 13. ACS Med Chem Lett. 2023. PMID: 37077385 Free PMC article.
Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.
Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM. Galal KA, et al. Among authors: kramer a. bioRxiv [Preprint]. 2023 Dec 5:2023.12.04.569845. doi: 10.1101/2023.12.04.569845. bioRxiv. 2023. Update in: Bioorg Med Chem Lett. 2024 Feb 1;99:129617. doi: 10.1016/j.bmcl.2024.129617 PMID: 38106118 Free PMC article. Updated. Preprint.
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: kramer a. J Med Chem. 2024 Jul 25;67(14):12261-12313. doi: 10.1021/acs.jmedchem.4c00962. Epub 2024 Jul 3. J Med Chem. 2024. PMID: 38959455 Free PMC article.
Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.
Gerninghaus J, Zhubi R, Krämer A, Karim M, Tran DHN, Joerger AC, Schreiber C, Berger LM, Berger BT, Ehret TAL, Elson L, Lenz C, Saxena K, Müller S, Einav S, Knapp S, Hanke T. Gerninghaus J, et al. Among authors: kramer a. J Med Chem. 2024 Aug 8;67(15):12534-12552. doi: 10.1021/acs.jmedchem.4c00411. Epub 2024 Jul 19. J Med Chem. 2024. PMID: 39028937
3,096 results