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Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity.
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. bioRxiv [Preprint]. 2024 Feb 18:2024.02.18.580805. doi: 10.1101/2024.02.18.580805. bioRxiv. 2024. Update in: J Med Chem. 2024 Aug 8;67(15):12534-12552. doi: 10.1021/acs.jmedchem.4c00411 PMID: 38405908 Free PMC article. Updated. Preprint.