Patent ID: 6514687
Filing Date: 2003-02-04
Classification: C07D,C12Q,G01N,Y10S

Abstract:
A method for screening a candidate compound for activity as a substrate of at least one CYP450 enzyme, comprising the steps of:contacting a CYP450 enzyme with the candidate compound and a reagent compound having the structure: Yâ€”Lâ€”Q, â€ƒwherein: 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; and detecting an optical signal, if any, resulting from interaction of the reagent compound with the CYP450 enzyme.