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:

  1. LY3502970 (OWL833) (Chugai/Lilly clinical oral non-peptide GLP-1R GPCR partial agonist)
  2. S64315 (Servier selective clinical Mcl-1 protein-protein interaction (PPI) inhibitor)
  3. daridorexant (Idorsia clinical dual orexin receptor GPCR antagonist)
  4. “peptide 78” (Merck/UCB/Ra Pharma macrocyclic PCSK9 protein-protein interaction (PPI) inhibitor)
  5. BMS-986144 (Bristol-Myers Squibb (BMS) pan-genotype HCV NS3/4A protease inhibitor)
  6. MLT-985 (Novartis allosteric MALT1 protease (paracaspase) inhibitor)
  7. EB-42486 (ESCAPE Bio oral G2019S-LRRK2 mutant-selective kinase inhibitor)
  8. “compound 4d” (Merck oral selective PI3K delta kinase inhibitor)
  9. “compound 60b” (Taisho D486N mutant RSV fusion protein inhibitor clinical candidate)
  10. “compound 15a” (Novartis reversible in vivo ATX inhibitor)
  11. “compound 31” (Merck cholesteryl ester transfer protein (CETP) inhibitor)
  12. “compound 36” (GlaxoSmithKline (GSK) oral TRPV4 ion channel antagonist backup)
  13. BCPyr (Pfizer cIAP1-based BTK degrader)
  14. “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.