This was a loaded month for pioneering drug discovery programs! Among the highlights are a reversible-covalent inhibitor from Novartis, the hotly followed SHP2 inhibitor from Novartis, several innovative compounds from Pfizer including an oral GLP-1R agonist with a cryo-EM structure, a liver-targeted ACC inhibitor, and an oral KHK inhibitor. Remarkably, half of the molecules are …
Plenty of eye-opening material was published this August! Among this month’s highlights are a small molecule with twice-a-year dosing from Gilead, a non-classical C-H—O hydrogen-bonding kinase inhibitor from Pfizer, an E1 ligase inhibitor with a cool substrate-assisted covalent mechanism from Takeda, and some STING agonists with well-tolerated oral activity and fascinating mechanisms from Merck and …
Many more modalities, mechanisms, screening strategies, and interesting chemical motifs appeared from the drug discovery community in July. This time we have a compound from a DNA-encoded library screen, some compounds derived from phenotypic screens, and a starting point identified from a high-throughput mass screen. We also have the first cryo-EM structure featured this year …
The drug discovery community kicked off the summer with a lot of very interesting molecules published in June. After ~50 molecular highlights so far this year, you’d think we’ve seen it all, but there were again numerous fascinating chemical motifs, molecular mechanisms, and biological observations disclosed last month. In this group are some natural-product inspired …
Here’s May’s round-up of small molecule highlights, with comments and links to articles below. There was a lot of diversity among targets last month, although there were surprisingly few structure-based campaigns disclosed. Plenty of interesting biology and chemical structures to consider! eFT226 (zotatifin) is a beautiful natural product-derived molecule that inhibits the RNA helicase eIF4A …
April 2020 was another great month for drug discovery publications, with several interesting first disclosures of clinical candidates and a variety of uncommon chemical motifs that will pique most chemists’ interest. Here’s a visual summary of the molecules, with some comments and links to the articles below: Tucatinib is the third approved HER2 kinase inhibitor …