Substrate Specificity and Overlap

TABLE 9.3. Characteristics of Human P450 Substrates of Families CYP1, CYP2, and CYP3 [Pg.156]

0/ /o Drugs CYP Range of log P Values Average log P Value (n) Other Characteristics Typical Substrate and log P [Pg.156]

3 1A1 1.39-6.35 3.41 [16] Planar PAHs and their diols DMBA-3,4-diol 3.42 [Pg.156]

Potentially important discriminants of P450 selectivity include size (diameter), molecular mass or length of the molecule, planarity (aid1) or rectangularity (II w) of the molecule, lipophilicity (log P or log D 7.4), basicity/acidity of the compound (pAa), polarity (dipole moment) of the molecule, and compound lipophilicity for substrate binding to human P450s in drug metabolism. [Pg.156]

Source Lewis, D. F. V., Jacobsa, M. N., and Dickins, M. Drug Discovery Today 9, 530-537, 2004. [Pg.156]

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