The September edition of Small Molecules of the Month, features a number of fascinating molecules and mechanisms, including a beta-lactamase inhibitor optimized to have single agent antibiotic activity, a biased agonist of S1P1 that minimizes receptor internalization in favor of GCPR agonism, an oral AR degrader similar to ARV-110 and a molecule that unfortunately demonstrates QTc prolongation in vivo without a significant in vitro signal. Special thanks to reviewer Mike Koehler for commentary on the cover molecule, ETX0462, this month.