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Posts tagged with "Drug Assays"

  • Analytical Chemistry

    More on Covalent Compounds, And Covalent Fragments

    At a previous company some years back, I was interested in getting a “covalent fragment” collection going, and did to a small extent. It got screened against some antibacterial targets, but never became all that popular. That was partly because fragment-based screening was a younger field, and combining it with covalent drug discovery … Read More
  • Analytical Chemistry

    Fragment Binding, All the Way Down

    I remember the time before anyone did fragment-based drug discovery, when I heard high-micromolar binding ligands described as “carpet lint” or “stuff from the bottom of your shoe”. And you only heard then when the assays themselves even read out at that level, which certainly wasn’t a given. When I started, a suggesti… Read More
  • Drug Assays

    Down Amongst the Water Molecules

    This new paper shows one reason why it’s so tricky to calculate compound binding in an active site (which is what we’d want to do in order to do effective in silico virtual screening). The authors (a multicenter team from York, Demuris, Vernalis, and St. Jude) are looking at a virulence protein from H. influenzae… Read More
  • Clinical Trials

    What’s Crucial And What Isn’t

    One of the reasons that people in or near this business can write such gaudy press releases is that it has so many moving parts. That lets everyone claim that the part that they’re addressing is Crucial. Think of a car: the wheels are indeed key to mobility, but so is the engine. As is… Read More
  • Chemical Biology

    Probes For Everything

    In case you don’t know, there’s officially an effort to try to develop chemical probes for basically every protein in the human proteome. The “Target 2035” initiative has been looking through the literature and finding what you’d expect: power-law distributions that have most people working on proteins that other peopl… Read More
  • Cancer

    Your Cancer Targets May Not Be Real

    I wrote here about a paper from Cold Spring Harbor labs that invalidated MELK as a cancer target. That was straightforward enough: knocking it out via CRISPR across a whole range of cancer cell lines had no effect on their growth at all, so it’s kind of hard to make the case that it’s an… Read More
  • Drug Assays

    How Close Do You Get to the Best Compound?

    Here’s a topic that came up in my Twitter feed the other day – I fear it’s unanswerable, but I’d like to hear what people have to say about it. Drug discovery projects start, of course, from a selection of possible chemical matter and chemical series, and they eventually narrow down to a clinical candidate. Read More
  • Drug Assays

    Has AI Discovered a Drug Now? Guess.

    Here is an interesting paper in Nature Biotechnology on computational drug design, and if you read it without reading any of the accompanying articles about it, you will have a perfectly good time. There are things that you will be impressed by, and there are things that you will argue with, but that’s how most papers… Read More
  • Chemical News

    Not All Of Those Compounds Are Real. Again.

    The Nrf2 pathway has been a hot area of research for some years now, particularly in oncology. It’s a basic-leucine-zipper transcription factor that under normal conditions stays mostly out in the cytosol, where it’s under tight regulatory control. Under cellular stress, though, it heads into the nucleus and fulfills its transcription-f… Read More
  • Drug Assays

    Phenotypic Neuroscience

    This is a good review from AstraZeneca scientists on phenotypic screening in neurodegenerative disease (by which one means Parkinson’s, Huntington’s, frontotemporal dementia, Lewy body dementia, and of course Alzheimer’s). And it’ll serve as a good intro to the challenges in these two fields in general, and to why they inter… Read More
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