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As ADME assays are performed earlier in drug discovery, the numbers of test compounds increases as does the need for predictive assays that are rapid, sensitive, cost effective and simple to perform. A novel bioluminescent assay format will be described that overcomes conventional limitations concerning one or more of these criteria. The simple add and read approach employs luciferase pro-substrates as activity probes for drug metabolizing enzymes that convert them to a product that generates light with luciferase in direct proportion to the enzyme activity of interest. An extensive collection of these drug-like probes with selectivity for a wide range of enzymes has now been synthesized. They are used in several cytochrome P450 (CYP), monoamine oxidase, N-acetyl transferase, UDP glucuronosyl transferase (UGT) and glutathione transferase (GST) assays. Cell free biochemical assays are used to screen for enzyme specific inhibitors and cell based CYP assays are used to measure induction in hepatocytes. The luminogenic assays produce IC50s for enzyme inhibition and EC50s for CYP induction that correlate well with conventional assays in terms of rank order and absolute potency. The cell-based CYP3A4 enzyme assay is compatible with orthogonal measurements such as CYP1A2, CYP3A4 transcriptional induction and cell viability. These multiplex approaches stream line data collection while improving data quality,
strengthening interpretation and removing ambiguity. This bioluminescent ADME assay suite provides an efficient approach to the discovery phase of drug development.

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