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    • 4. 发明公开
    • ACTIVITY-BASED PROBE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE
    • EP4310504A2
    • 2024-01-24
    • EP23207737.0
    • 2017-12-23
    • The Board of Trustees of the Leland Stanford Junior University
    • BOGYIO, Matthew, S.VERDOES, Martijn
    • G01N33/68
    • The present invention relates to a compound for use in labeling a protease having the formula (II):

      wherein D comprises a benzoindole dye; L 1 is a linker; AA 1 is an amino acid side chain; U is O, NH, or S; R 1 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, or a protecting group, and is optionally substituted with 1 to 3 A groups; each A is independently alkyl, alkenyl, alkynyl, alkoxy, alkanoyl, alkylamino, aryl, aryloxy, arylamino, aralkyl, aralkoxy, aralkanoyl, aralkamino, heteroaryl, heteroaryloxy, heteroarylamino, heteroaralkyl, heteroaralkoxy, heteroaralkanoyl, heteroaralkamino, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkoxy, cycloalkanoyl, cycloalkamino, heterocyclyl, heterocyclyloxy, heterocyclylamino, heterocyclylalkyl, heterocyclylalkoxy, heterocyclylalkanoyl, heterocyclylalkamino, hydroxyl, thio, amino, alkanoylamino, aroylamino, aralkanoylamino, alkylcarboxy, carbonate, carbamate, guanidinyl, urea, halo, trihalomethyl, cyano, nitro, phosphoryl, sulfonyl, sulfonamido, or azido, L 3 is a linker; and Q comprises a quencher, and wherein the benzoindole dye has the structure:

      wherein o is an integer from 1 to 4; R 2 is a C 2 -C 8 alkyl group, optionally substituted with a sulfonate or carbonate; each R 3 is independently a C 1 -C 6 alkyl group; and L 4 is an optionally substituted alkyl linker, wherein each carbon atom is optionally replaced with a heteroatom.