With the all the newsflow on drug re-purposing for the coronavirus, it’s easy to overlook all the interesting drug discovery articles that have been published in March. A summary of some of the most interesting compounds that appeared online this month appears below, and links to the original articles are at the bottom. Two molecules with degrader mechanisms that demonstrated compelling in vivo activity made this month’s list, and a flurry of excellent molecules intended for hot (or once hot) oncology targets appeared as well.

Small Molecules of the Month - Mar. 2020

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Links to Articles:

  1. CC-92480 (Celgene/Bristol Myers Squibb (BMS) oral in vivo CRBN-based selective IKZF1/3 degrader)
  2. “PROTAC 6” (GlaxoSmithKline (GSK) IAP-based selective RIPK2 degrader with prolonged in vivo PD)
  3. GSK620 (GlaxoSmithKline (GSK) oral in vivo BD2 domain selective BET inhibitor)
  4. Merck hArg1 inhibitor (Merck oral in vivo human arginase 1 inhibitor)
  5. Merck IDO1 inhibitor (Merck heme-displacing oral IDO1 inhibitor)
  6. Constellation EZH2 inhibitor (Constellation oral in vivo long-residence time EZH2 inhibitor)
  7. Arcus CD73 inhibitor (Arcus non-nucleoside CD73 inhibitor)
  8. MK-6884 (Merck M4 positive allosteric modulator PET tracer)
  9. Sulfopin (Weizmann/Harvard selective covalent Pin1 inhibitor)
  10. M3814 (Merck KGaA oral DNA-PK selective kinase inhibitor)
  11. Remibrutinib (Novartis oral BTK-selective covalent kinase inhibitor clinical candidate)

A few other molecules from the same time frame I thought were interesting but couldn’t squeeze into the figure:

More Molecules:

  • “Compound 34” – an orally bioavailable N-sulfoximineurea NLRP3 inflammasome inhibitor
  • TZH-P1-2 – a covalent inhibitor of the PI5P4K lipid kinase family targeting a cysteine on a disordered loop
  • “Compound 1” – an FGFR4 covalent inhibitor from BMS
  • “Compound 5a” – an RORgt inverse agonist from Teijin Pharma and Amgen
  • KL101 and TH301 – CRY1/2 modulators from Nagoya that enhance brown adipocyte differentiation

Happy quarantining! Explore drughunter.com for more.