It’s hard not to think about infectious diseases at the moment, but it’s a great time to review the drug discovery literature. One area of drug discovery that has deep roots in infectious disease research is targeted covalent inhibition. Targeted covalent inhibitors form covalent bonds with discrete targets (as opposed to non-specific modifiers like nitrogen …
Of the 2019 biotech IPOs on the major US exchanges, there were 24 companies focused on developing non-small molecule drugs, about the same number as those developing small molecule drugs. Here’s a list of the companies (by market cap at IPO) along with a short summary of the key concepts for each company’s main programs. …
Of the 2019 biotech IPOs on the major US exchanges, 25 companies are focused on discovering and developing small molecule drugs. Here’s a list of the companies (by market cap at IPO, top to bottom) along with the main mechanisms of action of the lead molecules and other publicly disclosed targets. The largest company by …
This guest post introduces the Topliss schemes for analog synthesis, illustrates when they might be useful, and provides easy-to-use “cheat sheets” of the original schemes. Imagine you’re on a new project that has just conducted a chemical screen on a novel target, and you’re excited to see a few micromolar hits. You want to develop …
or, How I Learned to Stop Worrying and Love My Own Definition. Recently I posted on “biologic drugs” which were approved in 2019. All was well in my little scientific universe, until I received this in an email: “You recently reported “14 novel biologic drugs,” referring to ‘novel’ biopharmaceuticals approved CDER. But, … You also …
Jump to Cheat Sheet Lipophilicity is a drug discovery concept that I didn’t take seriously enough when I first started. It made me focus on the wrong molecules and caused me to design and synthesize buckets of compounds that in retrospect were clearly headed nowhere. This post is here to save you that time. If …