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. Author manuscript; available in PMC: 2020 Nov 27.
Published in final edited form as: J Med Chem. 2019 Nov 11;62(22):10391–10401. doi: 10.1021/acs.jmedchem.9b01485

Figure 1.

Figure 1.

First generation of VFV derivatives. Although log P > 5 and mol wt > 500 are “violations of Lipinski’s rule of five”, there are numerous examples of successful drugs with larger values, especially those aimed at intracellular membrane-bound targets (e.g., cinacalcet/Sensipar at a log P of 6.5 and systemic clinical drug inhibitors of microbial CYP51 such as itraconazole (log P = 6.8, mol wt = 704) and posaconazole (log P = 5.5, mol wt = 701)).