Hope everyone had a fantastic Christmas weekend. Last month there were quite a few large small molecules, including three macrocycles. Quite a few of these molecules would’ve made for a decent synthesis PhD project! Some highlights include a cryo-EM structure for Chugai/Lilly’s GLP-1R agonist, a Ra Pharma mRNA display screen yielding a PCSK9 PPI inhibitor, …
Hope everyone is having a great US Thanksgiving week. This month’s update features quite a few contributions from international companies, including three from Bayer in Germany, a double soft drug from Leo Pharma in Denmark, and others from sites in Poland, Belgium, Spain, China, and India. Links to Articles: BAY 1214784 (Bayer oral hGnRH-R hormone …
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 …