Abstract: Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity.

Abstract: Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity. The compounds are particularly useful for assessing cytochrome P450 CYP3A enzyme activity.

Abstract: Novel fluorescent substrates of the human P450 enzyme CYP2D6 are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing CYP2D6 enzyme activity and in selecting compounds which inhibit CYP2D6 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of CYP2D6 enzyme activity.

Abstract: An improved method for measuring the activity of a promoter sequence in a mammalian cell using a reporter gene is provided. The improvement involves using a reporter cassette containing a DNA sequence encoding a cytochrome P450 with a polyadenylation signal sequence as the reporter gene. Compositions containing the cytochrome P450 reporter cassette also are provided.

Abstract: An immortal human cell line stably expressing a multiplicity of cytochrome P450s is provided. Preferably, the cell line is MCL-5, which stably expresses cytochrome P450 IA1, IA2, IIA3, IIIA4, and IIE1, as well as microsomal epoxide hydrolase. The cell line is useful in mutagenicity, toxicity and metabolism studies.

Abstract: The invention provides methods and products equal in a selection system for determining the presence or absence of a vector in a mammlian cell. The vector of the invention carries and is capable of expressing a gene encoding a protein capable of effecting the conversion of a precursor to an essential amino acid. A mammalian cell line is created with conditions capable of causing the vector to be introduced into the mammalian cell line. Then, the created mammalian cell line is grown in medium containing a precursors to the essential amino acid but not containing the growth-supporting amount of the essential amino acid and those cells capable of growing are selected.