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Along with the fact that MK-3903 is an enzyme activator, there are a number of different notable features about this story. First, despite the problem of the target, the group made speedy progress, shifting from the initial display screen to great tool compounds in lower than a 12 months. Second, as close to as I can tell, this optimization was done in the absence of direct structural data on how the compounds bind. (A publication by a separate team, who was closely monitoring the patent literature, describes the crystal construction and mechanistic evaluation of a associated molecule.) Third, all of this work stemmed from a single fragment: though extra ligandable targets may produce numerous hits, in the end you solely need one.
Lots of people make the mistakes of being too matchy-matchy with their room design. While some matching is all … Read More “Sauer & Steiner”