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. |