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Posts tagged with "Drug Assays"

  • Drug Assays

    Lilly’s Virtual Med-Chem Assistant

    Here’s an interesting new paper from Lilly (brought to my attention by Ash Jogalekar on Twitter). “Creating a virtual assistant for medicinal chemistry” is the title, but fear not: this is not something that’s come to elbow you aside at the bench. Well, not yet. What they’re talking about is a software agent that is… Read More
  • Chemical News

    The Cyclofluidic Story

    The recent post here on automation in chemistry (especially medicinal chemistry) is a good intro for this paper in ACS Med. Chem. Letters. It’s from David Parry, who led Cyclofluidic, and I’ve blogged about them a few times over the years. That was a company formed in 2008 in the UK to try to develop… Read More
  • Animal Testing

    Enough With the Mouse Behavioral Models?

    This piece in STAT is well worth a read. The author, Adam Rosenberg of Rodin Therapeutics, is ready to ditch rodent-centric models for human CNS disease, and I can see where he’s coming from. I’ve often said that when I think back on my Alzheimer’s and schizophrenia drug discovery days (back when I was first… Read More
  • Chemical Biology

    Making Some New Compounds, to Fit Some New Receptors

    Here’s some medicinal chemistry combined with synthetic biology for you. Many people are used to thinking in terms of finding small-molecule probes for various cell targets, and those are valuable things. But what if you want to control a certain population of (for example) ion channels, but there aren’t any compounds that will do the… Read More
  • Cancer

    Making and Measuring Multivalency

    Here’s an unusual paper that’s studying receptor behavior on cell surfaces by use of atomic force microscopy. (Here’s the SI file, which is free to access). The authors took the marketed VEGF inhibitor vandetanib (VD6474) and attached it through linkers to the AFM tip, and then scanned around the surface of live human umbilical v… Read More
  • Drug Assays

    Comparing Compound Collections

    A common question – well, it should be a common question, anyway – is “How do I make sure that this compound collection is a useful one to screen?” There are alternative forms that come down to the same issues – if you’re putting together a new focused screening set, what should be in it?… Read More
  • Analytical Chemistry

    A Close Look at Fragments

    Here’s a look from the D. E. Shaw research team at fragment binding, and even if you don’t do fragment-based drug discovery, it’s worth a read. That’s because the mechanisms by which fragments bind to proteins are most likely the fundamental ones by which larger molecules bind as well; this is the reductionist look at… Read More
  • Chemical Biology

    What Those Degraders Are Actually Doing

    Since targeted protein degradation is such a hot topic these days, this paper (which adds to the results obtained by this one) should get some interest. It’s a report of a detailed look at the kinetic behavior of several bifunctional degraders – and there’s a lot of kinetic behavior to look at. That’s because you’re l… Read More
  • Drug Assays

    Experiences With Phenotypic Screening?

    Very little blogging time today, but I wanted to throw a question out to the readership instead. I’m at the Keystone conference on Phenotypic Drug Discovery, so here’s a relevant topic: what are your own experiences with phenotypic screening? Background for those outside the field: broadly speaking, you can sneak up on a drug by… Read More
  • Biological News

    Targeting microRNAs

    Medicinal chemists spend the vast majority of their time targeting proteins. Enzyme active sites, receptors, allosteric sites, interfacial sites – it’s one protein after another, to the point that you can mentally assume that your compounds are going to be hitting the familiar landscape of backbone amide bonds, pi-interacting tryptophan… Read More
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