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, and a crystal structure of a BTK-degrader-cIAP ternary complex from Pfizer. Enjoy!
Small Molecules of the Month - Nov. 2020
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Links to Articles:
- LY3502970 (OWL833) (Chugai/Lilly clinical oral non-peptide GLP-1R GPCR partial agonist)
- S64315 (Servier selective clinical Mcl-1 protein-protein interaction (PPI) inhibitor)
- daridorexant (Idorsia clinical dual orexin receptor GPCR antagonist)
- “peptide 78” (Merck/UCB/Ra Pharma macrocyclic PCSK9 protein-protein interaction (PPI) inhibitor)
- BMS-986144 (Bristol-Myers Squibb (BMS) pan-genotype HCV NS3/4A protease inhibitor)
- MLT-985 (Novartis allosteric MALT1 protease (paracaspase) inhibitor)
- EB-42486 (ESCAPE Bio oral G2019S-LRRK2 mutant-selective kinase inhibitor)
- “compound 4d” (Merck oral selective PI3K delta kinase inhibitor)
- “compound 60b” (Taisho D486N mutant RSV fusion protein inhibitor clinical candidate)
- “compound 15a” (Novartis reversible in vivo ATX inhibitor)
- “compound 31” (Merck cholesteryl ester transfer protein (CETP) inhibitor)
- “compound 36” (GlaxoSmithKline (GSK) oral TRPV4 ion channel antagonist backup)
- BCPyr (Pfizer cIAP1-based BTK degrader)
- “compound 4j” (Janssen (JNJ) brain-penetrant in vivo 5-HT2 antagonist and 5-HT7 inverse agonist, backup candidate)
Hope this was helpful, and have a great new year. Explore drughunter.com for more.
