1-Aminocyclobutanecarboxylic acid exhibits multi-faceted bioactivity across various assays. It shows in vitro inhibition of glycine at the NMDA receptor with an IC50 of 19,000 nM, and specifically in oocytes with an IC50 of 18,500 nM. In rat brain cortex membranes, it acts as a partial agonist at the glycine site of the NMDA receptor, potentiating [3H]Mk-801 binding by 53.0% relative to glycine in the presence of 5,7-dichlorokynurenic acid, and displaces [3H]glycine with a Ki value of 15,848.93 nM.
Beyond its effects on NMDA receptors, 1-Aminocyclobutanecarboxylic acid is notable for its inhibitory actions on several bio-targets: it inhibits the Menin-MLL interaction pivotal in MLL-related leukemias with a potency of 39,810.7 nM, Tau fibril formation and Thioflavin T binding at 12,589.3 nM, Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) at 79,432.8 nM, and Anthrax lethal toxin internalization at 12,589.3 nM. It also displays activity in the Cytochrome p450-cyp1a2 panel assay with an AC50 of 39,810.72 nM.
Additionally, 1-Aminocyclobutanecarboxylic acid significantly inhibits sodium fluorescein uptake in OATP1B3- and OATP1B1-transfected CHO cells, showing 95.93% and 131.14% inhibition respectively at a 10 µM substrate-inhibitor concentration, indicating potent effects on these transporters. Lastly, it inhibits ASCT2-mediated [3H]-D-serine uptake in rat hippocampal astrocytes at 1 mM concentration, reducing uptake by at least 25.0% within 5 minutes..
Note: Summary generated by AI. Data source: ChEMBL 