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  How to Get Drugs Into the Brain

  By Dennis KoesterReviewed and edited by Michael Walters and Dennis Hu Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter Flash Talk. Here, he sums up some key points on how to find compounds…

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  Drug Target Identification Methods After a Phenotypic Screen

  Here’s a common scenario – your team has just completed a phenotypic screening campaign, cleaned out the false positives through hit triage, and now you have modestly optimized validated leads with cell-based activity. The problem is, you have no idea how your compounds work, and whether they act on a target or set of targets…

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  Phase II Drug Metabolism

  This article explains what Phase II drug metabolism is, contains a poster summarizing common enzyme-mediated bioconjugation reactions, and provides interesting examples of Phase II transformations and their impact on drug pharmacology. “As any biotransformation scientist will know, metabolism is not a binary function, and drugs can be cleared through multiple mechanisms,” says Dr. Julia Shanu-Wilson…

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  What Makes a Drug Best-in-Class?

  How a Follow-on Drug Can Create Value After a First-in-Class Drug Novel drugs can make a big impact in two main ways—by being first-in-class (FIC) or by being best-in-class (BIC). A novel drug that produces its therapeutic effect by interacting with a new target or that is used to treat a new condition is considered…

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  Minimum Viable Experiments with Imperfect Molecules: a Minipump Minireview

  Optimizing lead compounds to have drug candidate-like qualities are time-consuming and expensive. Oftentimes, critical drug discovery project questions, such as on-target pharmacology or toxicology, can be answered more efficiently with compounds that are “good enough,” saving teams time and further resource investment. This article discusses tools and strategies available to get desired in vivo pharmacology…

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  Why pKas Matter in Medicinal Chemistry and a Drug Discovery Amine pKa Table

  In this article, we highlight the importance of pKa values in medicinal chemistry and drug discovery and provide a reference poster of pKa values of common amines’ conjugate bases. Since amines are often a part of marketed drugs, knowledge of their pKas can provide guidance in the selection of basic moieties to match the desired…