A potential first-in-class drug for NASH, a mutant-selective degrader of PI3Ka, and a bi-steric inhibitor of mTOR are some examples of this month's MOTM. Learn more about the molecules by navigating t...

After evaluating thousands of articles and hundreds of candidates, a brain-penetrant pre-mRNA splicing modulator, a gut-restricted candidate for Parkinson’s disease (you read that correctly), and a ma...

Ten of the most interesting and instructive small molecule case studies that appeared in the literature in Oct. 2022 are shown below. Learn more about the molecules by navigating to the full reviews o...

Click on each molecule on the right to find its recent publication and view the Premium deep dive which covers: why the molecules matter, how they were discovered, the key steps behind optimization, h...

A covalent KRASG12R inhibitor used as a proof-of-concept for covalent arginine modification, an oral dihydroorotate dehydrogenase inhibitor being developed for acute myelogenous leukemia, and a first...

An oral, brain penetrant EGFR mutant inhibitor with exquisite selectivity, a drug that was originally developed from a brain cholesterol metabolite, and a muscarinic antagonist and β2 agonist that was...

A SETD2 inhibitor with Fast Track Status for hematological malignancies, a CNS-penetrating, ATP-competitive LRRK2 inhibitor for Parkinson’s disease, and an oral nonsteroidal mineralocorticoid receptor...

A fat-tissue-targeting clinical candidate, a first-in-class Ph. III molecule that inhibits its target by covalently modifying the target’s substrate, and a fourth-generation glucokinase activator are...

Drug Hunter’s April 2022 edition of Molecules of the Month features some emerging small molecule clinical candidates as well as several interesting molecules in preclinical stages for a broad range of...

This month's edition of Drug Hunter's Molecules of the Month include Principia's reversible covalent BTK inhibitors and a single-dose antimalarial. Thanks to Bryan McKibben, Dennis Koester, Callie Bry...

Drug Hunter’s February 2022 Small Molecules of the Month include a glucokinase partial activator, an orexin receptor agonist intended to promote wakefulness rather than sleep, and an orally available...

In 2022, Drug Hunter highlighted 120 Molecules of the Month with structures or stories that were published for the first time, were approved or disclosed new significant data. They were selected from...

The January 2022 edition of Drug Hunter’s Small Molecules of the Month includes a reversible CoV-2 main protease inhibitor from Shionogi in Ph. II/III which doesn’t require a PK booster like ritonavir...