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
send download link to:
Links to Articles:
- LNP023 (Novartis (NIBR) oral in vivo retinal barrier penetrant selective factor B serine protease inhibitor)
- LMB763 (nidufexor) (Novartis (GNF) oral in vivo selective FXR partial agonist)
- ABBV-744 (AbbVie oral in vivo BD2 domain selective BET inhibitor)
- AG-881 (vorasidenib) (Agios oral brain penetrant allosteric mutant IDH1/2 dual inhibitor clinical candidate)
- FT-2102 (olutsidenib) (FORMA oral allosteric mutant-selective IDH1 inhibitor clinical candidate)
- GS-9876 (lanraplenib) (Gilead Sciences oral SYK selective kinase inhibitor clinical candidate)
- KRAS(G12C) inhibitor from AZ (AstraZeneca oral in vivo mutant KRAS(G12C) allosteric covalent inhibitor)
- RORγt inhibitor from Merck (Merck ROR-gamma-t oral in vivo allosteric inhibitor)
- WF-47-JS03 (Novartis (GNF) oral in vivo RET kinase inhibitor)
- BMS-986260 (Bristol Myers Squibb (BMS) oral in vivo selective TGF-beta-R1 kinase inhibitor)
- 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:
- “Compound 12” – Reversible inhibitor of endothelial lipase (EL) selective against hepatic lipase (HL) that demonstrates HDL-C increases in vivo from Bristol-Myers Squibb.
- 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.
- “Compound 21” – a CNS-penetrant ASK1 kinase inhibitor from Biogen, derived by modifying the solvent-exposed region of prior ASK1 inhibitors.
- “Compound 29” – a potent allosteric inhibitor of HIV-1 integrase from Bristol-Myers Squibb.
- “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.