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Posts tagged with "Drug Assays"

  • Drug Assays

    The Hideous Numbers of Compounds

    I was blithely throwing around the term “chemical space” in yesterday’s post. So, what am I talking about, and how much room is in there, anyway? Let’s narrow it down to organic compounds, to start with, or at least compounds that are mostly organic. A working definition, as far as people interested in biology and… Read More
  • Chemical News

    Diversity-Oriented Synthesis: Oriented The Right Way?

    Ever hear of Diversity-Oriented Synthesis? It’s an odd bird. DOS tries to maximize the number of structures and scaffolds produced from a given synthetic scheme – to find the most efficient ways to populate the largest amount of chemical space. In a way, it’s the contrapositive of natural product synthesis, which focuses all its effort… Read More
  • Drug Assays

    Sticking It to Proteins

    So, you’re making an enzyme inhibitor drug, some compound that’s going to go into the protein’s active site and gum up the works. You usually want these things to be potent, so you can be sure that you’ve knocked down the enzyme, so you can give people a tiny, convenient pill, and so you don’t… Read More
  • Biological News

    Wash Your Tubes; Mess Up Your Data

    I wrote a while back about the problem of compounds sticking to labware. That sort of thing happens more often than you’d think, and it can really hose up your assay data in ways that will send you running around in circles. Now there’s a report in Science of something that’s arguably even worse. (Here’s… Read More
  • Animal Testing

    Animal Models: How High to Set the Bar?

    A key step in all drug discovery programs are the cellular and animal models. The cells are the first time that the compounds are exposed to a living system (with cellular membranes that keep things out). The animals, of course, are a very stringent test indeed, with the full inventory of absorption, metabolism, and excretion… Read More
  • Analytical Chemistry

    X-Ray Structures: Handle With Care

    X-ray crystallography is wonderful stuff – I think you’ll get chemists to generally agree on that. There’s no other technique that can provide such certainty about the structure of a compound – and for medicinal chemists, it has the invaluable ability to show you a snapshot of your drug candidate bound to its protein target. Read More
  • Biological News

    Receptors: Can’t Live With ‘Em, Can’t Understand ‘Em

    At various points in my drug discovery career, I’ve worked on G-protein-coupled receptor (GPCR) targets. Most everyone in the drug industry has at some point – a significant fraction of the known drugs work through them, even though we have a heck of a time knowing what their structures are like. For those outside the… Read More
  • Business and Markets

    Sharing the Enlightenment

    Here’s an interesting idea: Merck, Lilly, and Pfizer are bankrolling a startup company to look for new technologies for drug development. Enlight Biosciences will focus on the biggest bottlenecks and risk points in the process, including new imaging techniques for preclinical and clinical evaluation of drug candidates, predictive toxicology a… Read More
  • Drug Assays

    Oops

    We recently encountered a problem that’s (unfortunately) a rather common one. An enzyme assay turned up an interesting hit compound, with some characteristics that we were hoping to see for leads against our target. A re-test showed that yes, the activity appeared to be real, which was interesting, since this hit was a welcome surprise… Read More
  • Drug Assays

    The Miracle Solvent

    For those who were wondering, my copper reactions the other day worked out just fine. They started out a beautiful blue (copper iodide and an amino acid in straight DMSO – if that’s not blue it’s maybe going to be green, and if it’s not either one you’ve done something wrong). Of course, the color… Read More
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