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Posts tagged with "Drug Assays"

  • Chemical News

    New Reactions And Where They’ll Come From

    Here’s a new paper calling for expanding the medicinal chemistry synthetic toolbox. There have been calls like this before, of course, but those weren’t wrong, either. It’s not hard to figure out how we’ve ended up where we are, though (links added to replace footnotes in the below paragraph): The limited set of reaction typ… Read More
  • Chemical Biology

    In Situ Click Chemistry For Antibiotics

    I have always had a liking for the technique of having target proteins assemble their own inhibitors. This goes under several names: target-guided synthesis or protein-templated reactions more generally, and in situ click chemistry when the triazole/alkyne reaction is used as the assembly method. But the idea is the same in each case. You bring… Read More
  • Biological News

    GPCRs: Peeling The Onion Some More

    I like to say that when I was first working on G-protein coupled receptors (GPCRs) as drug targets, that after I while I thought I really understood a lot of what was going on. But that was the peak. Further experience eroded that confidence, and even though I’ve learned a lot more about them over… Read More
  • Analytical Chemistry

    How Close is Cryo-EM To Riding Over the Horizon?

    OK, all this cryo-electron microscopy stuff is great, new protein structures, things that are huge, that can’t be crystallized, fine, fine: but when, the medicinal chemists in the audience ask, will we be able to use it for structure-based drug discovery? This new review tries to answer just that question. The first thing that you… Read More
  • Chemical Biology

    Only Bind

    Here’s a new piece by Stuart Schreiber that lays out a shift in thinking that many people in the chemical biology field have been experiencing over the last few years. Medicinal chemists are used to making functional drug candidates – and by “functional” I mean compounds that make protein targets do something. For an enzyme… Read More
  • Drug Assays

    PAINs Filters In the Real World

    Here’s a look (open access) at Eli Lilly’s screening collection in terms of PAINS filters, and there are things for everyone to argue about in it. The entire concept of these filters has been occasion for argument, of course. Allow me to caricature some of the opinions that you hear in these: at one extreme, it… Read More
  • Drug Assays

    Combination Screening, Scaled Up

    Here’s another one for the Brute Force File, always noting that brute repetitious force is what machines are here for. A joint MIT/Broad Institute effort reports on a platform for combinatorial drug screening in nanodroplets, in this case looking for known compounds that potentiate the effect of antibiotics on gram-negative bacteria. Testing… Read More
  • Analytical Chemistry

    Looking Way Down Into the Cells

    Pharmacokinetics – the study of how drugs are taken up, distributed, metabolized, and cleared – is obviously a key part of drug development. Every drug substance gets handled somewhat differently by the human body, and these differences can completely determine whether you’ve got an effective therapy or not. But the tools we have… Read More
  • Chemical News

    Relay Calculates Its Way Through

    Bloomberg has a feature on Relay Therapeutics, who are just a few blocks away from me (and where several former colleagues of mine work). It’s a nice writeup, and also features a (relatively rare) spotlight on David Shaw of D. E. Shaw research. He’s one of those guys that you’ve likely never heard of unless… Read More
  • Chemical News

    Silicon In Drug Molecules, Revisited

    Here’s an update to a post from last year about silicon in drug-like molecules. The Denmark group at Illinois has investigated a range of silicon-containing heterocycles, providing both synthetic routes into the (mostly unknown) structures, and looking at some basic pharmaceutically relevant properties. There’s a lot of work in this pap… Read More
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