Skip to Content

Posts tagged with "Drug Assays"

  • Drug Assays

    The European Lead Factory

    That’s what they’re calling this new initiative, so points for bravery. I wrote about this proposal here last year, and now more details have emerged. The good news is that the former Merck facilities (well, Organon via Schering-Plough) in Newhouse (Scotland) and Oss (the Netherlands) will be part of the effort, so those will be… Read More
  • Drug Assays

    All Those Drug-Likeness Papers: A Bit Too Neat to be True?

    There’s a fascinating paper out on the concept of “drug-likeness” that I think every medicinal chemist should have a look at. It would be hard to count the number of publications on this topic over the last ten years or so, but what if we’ve been kidding ourselves about some of the main points? The… Read More
  • Chemical Biology

    So How Does One Grow Beta-Cells?

    The short answer is “by looking for compounds that grow beta cells”. That’s the subject of this paper, a collaboration between Peter Schulz’s group, the Novartis GNF. Schultz’s group has already published on cell-based phenotypic screens in this area, where they’re looking for compounds that could be useful in re… Read More
  • Drug Assays

    Eating A Whole Bunch of Random Compounds

    Reader Andy Breuninger, from completely outside the biopharma business, sends along what I think is an interesting question, and one that bears on a number of issues: A question has been bugging me that I hope you might answer. My understanding is that a lot of your work comes down to taking a seed molecule… Read More
  • Drug Assays

    The Theology of Ligand Efficiency

    So in my post the other day about halogen bonds, I mentioned my unease at sticking in things like bromine and iodine atoms, because of the molecular weight penalty involved. Now, it’s only a penalty if you’re thinking in terms of ligand efficiency – potency per size of the molecule. I think that it’s a… Read More
  • Drug Assays

    Automated Ligand Design?

    There’s a paper out in Nature with the provocative title of “Automated Design of Ligands to Polypharmcological Profiles”. Admittedly, to someone outside my own field of medicinal chemistry, that probably sounds about as dry as the Atacama desert, but it got my attention. It’s a large multi-center contribution, but the princi… Read More
  • Drug Assays

    Metal Impurities Will Waste Your Time

    Here’s a paper on a high-throughput screening issue that everyone in the field should be aware of: metal impurities in your compounds. The group (from Roche) describes a recent experience, and I think that many readers will shiver in recognition: The hits were resynthesized, and close analogues were prepared for early structure−activity rel… Read More
  • Drug Assays

    How Many Good Screening Compounds Are There?

    So, how many good screening compounds are there to be had? We can now start to argue about the definition of “good”; that’s the traditional next step in this process. But there’s a new paper from Australia’s Jonathan Baell on this very question that’s worth a look. He and his co-workers have already called attent… Read More
  • Drug Assays

    Four Million Compounds to Screen

    There’s a new paper out that does something unique: it compares the screening libraries of two large drug companies, both of which agreed to open their books to each other (up to a point) for the exercise. The closest analog that I know of is when Bayer merged with/bought Schering AG, and the companies published… Read More
  • Drug Assays

    A Broadside Against The Way We Do Things Now

    There’s a paper out in Drug Discovery Today with the title “Is Poor Research the Cause of Declining Productivity in the Drug Industry? After reviewing the literature on phenotypic versus target-based drug discovery, the author (Frank Sams-Dodd) asks (and has asked before): The consensus of these studies is that drug discovery based on t… Read More