Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change
Flibanserin, a compound identified as BIMT-17, acts as a complete agonist at the serotonin 5-HT1A receptor, with a binding affinity (Ki) of 1 nM, while functioning as an antagonist at the 5-HT2A receptor with a 49 nM affinity. Flibanserin D4 represents a deuterium-labeled version of Flibanserin.