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. 2021 Feb 7;64(4):1856–1872. doi: 10.1021/acs.jmedchem.0c01886

Figure 3.

Figure 3

Chemical properties impact ease of formulation. Generally, the more potent the compound the more facile the formulation. There are relatively routine procedures to formulate high melting or poorly water-soluble materials, but high melting poorly soluble crystals are a challenge. This problem was addressed by synthesis to increase potency on the human target enzyme, increase water solubility, and reduce the stability of the crystal structure.