A lot of very interesting drug discovery campaigns have already been published online this year. A summary of some of the resulting small molecules that I found most interesting appears below, including several clinical candidates and many fit-for-purpose biological tool compounds to assess efficacy and toxicity. Grab a coffee and use this post as a starting point in getting caught up on the literature this year! Links to the original articles below.

Small Molecules of the Month - Feb. 2020

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Links to Articles:

  1. LNP023 (Novartis (NIBR) oral in vivo retinal barrier penetrant selective factor B serine protease inhibitor)
  2. LMB763 (nidufexor) (Novartis (GNF) oral in vivo selective FXR partial agonist)
  3. ABBV-744 (AbbVie oral in vivo BD2 domain selective BET inhibitor)
  4. AG-881 (vorasidenib) (Agios oral brain penetrant allosteric mutant IDH1/2 dual inhibitor clinical candidate)
  5. FT-2102 (olutsidenib) (FORMA oral allosteric mutant-selective IDH1 inhibitor clinical candidate)
  6. GS-9876 (lanraplenib) (Gilead Sciences oral SYK selective kinase inhibitor clinical candidate)
  7. KRAS(G12C) inhibitor from AZ (AstraZeneca oral in vivo mutant KRAS(G12C) allosteric covalent inhibitor)
  8. RORγt inhibitor from Merck (Merck ROR-gamma-t oral in vivo allosteric inhibitor)
  9. WF-47-JS03 (Novartis (GNF) oral in vivo RET kinase inhibitor)
  10. BMS-986260 (Bristol Myers Squibb (BMS) oral in vivo selective TGF-beta-R1 kinase inhibitor)
  11. GNF2133 (Novartis (GNF) oral in vivo GSK3-beta-sparing DYRK1A kinase inhibitor)

If you’ve still got time, here are a few other molecules from the same time frame I thought were interesting but couldn’t squeeze into the figure:

More Molecules:

  1. “Compound 12” – Reversible inhibitor of endothelial lipase (EL) selective against hepatic lipase (HL) that demonstrates HDL-C increases in vivo from Bristol-Myers Squibb.
  2. SUVN-911 – A potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist which completed Ph. I in healthy volunteers. Interesting it is an antagonist though it is structurally similar to ABT-089, a partial agonist.
  3. “Compound 21” – a CNS-penetrant ASK1 kinase inhibitor from Biogen, derived by modifying the solvent-exposed region of prior ASK1 inhibitors.
  4. “Compound 29” – a potent allosteric inhibitor of HIV-1 integrase from Bristol-Myers Squibb.
  5. “Compound 47” – a orally available DprE1 enzyme inhibitor efficacious in a murine tuberculosis model.

Hope this is useful, and happy hunting! Explore drughunter.com for more.