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hGKRP-biotin was incubated with compound prior to addition of fluorescein-hGK and AlphaScreen beads (PerkinElmer). hGK-hGKRP binding was detected with Alphascreen fluorescein-detection beads in an EnVision Instrument (PerkinElmer).
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Achiral bis-trifluoromethyl and racemic methyl-trifluoromethyl carbinols have been established to be generally equipotent and are indistinctly used thorough our SAR discussions.
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84935887459
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Note the higher-lying (ca. 0.7 kcal/mol) undesired local minimum of the thiazole analog resides at a dihedral angle of ∼140, not 180, due to N-Cl repulsion.
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84935904070
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note
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Stereochemistry arbitrarily assigned.
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0033621044
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