Patent ID: 6638713
Filing Date: 2003-10-28
Classification: C07D,C12Q,G01N,Y10S

Abstract:
A kit for screening a candidate compound for activity as a substrate of at least one CYP450 enzyme, comprising:(a) an amount of a CYP450 enzyme, and (b) a reagent compound having the structure Y-L-Q, wherein: Y is selected from the group consisting of Q, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; wherein if Y is selected from Q, L is Lâ€², wherein Lâ€² is selected from the group of â€”(CR4H)(â€”OCR2H)p, wherein each R2 and each R4 is separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl and p is a positive integer no greater than twelve; L has the chemical structure Lâ€² or (â€”OCR2H)pâ€”, wherein each R2 is separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical means for generating an altered optical signal via cleavage of a Câ€”O bond; wherein the amount of the CYP450 enzyme in the well is sufficient to produce a detectable optical signal upon interaction with a portion of the reagent compound.