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. 2021 Sep;49(9):822–832. doi: 10.1124/dmd.120.000320

TABLE 5.

Parsing rationale for substrate and inhibitors

Category Clearance/P450-Glo Classification Parsing Rationale
1 +/+ Substrate Exhibiting activity in both assays, the compound is a clear ligand for the enzyme(s). It is unclear whether the parent, product, or both are responsible for the inhibition.
2 −/+ Inhibitor The compound is able to inhibit the enzyme metabolism of a probe substrate but is not itself cleared, indicating that the parent molecule is an effective inhibitor.
3 −/− Noncompetitor The lack of activity in both assays signifies either that binding does not occur or that the interaction does not generate a catalytically competent or inhibitory complex.
4 +/− Substrate Although a clear substrate, the binding kinetics of the parent compound and its metabolites do not preclude the concomitant metabolism of the P450-Glo probe.