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IC50 fluorescence polarization

In order to synthesize the all-small molecule PROT AC, it was advantageous to develop a more succinct method for the synthesis of Nutlin. A one-pot synthesis of a derivative of Nutlin-3 (13) was developed, as shown in Scheme 3.1. Following the synthesis of 13, it was verified by fluorescence polarization that this racemic derivative (modified for incorporation into a PROT AC) exhibited a similar ability to interact with MDM2 as the published Nutlin structures. It was observed that the IC50 of 13 was 21.4 pM, which is very similar to the reported IC50 for racemic Nutlin-3 of 13.6... [Pg.85]

IC50 measured in a competitive fluorescence polarization assay. 10 mM phosphate buffer (pH 7.4)... [Pg.608]

See other pages where IC50 fluorescence polarization is mentioned: [Pg.188]    [Pg.85]    [Pg.274]    [Pg.275]    [Pg.643]    [Pg.652]    [Pg.654]    [Pg.989]    [Pg.746]    [Pg.459]    [Pg.464]    [Pg.332]    [Pg.223]   
See also in sourсe #XX -- [ Pg.167 ]



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