Androgen receptorantagonist 1 is an orally available full androgen receptorantagonist (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.
Substance P ReceptorAntagonist 1 has the potential function in gastrointestinal disorders, inflammatory diseases, respiratory, and central nervous system disorders.
(E)-GABAB receptorantagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptorantagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
Adenosine receptorantagonist 1 is a highly selective antagonist for the A2aR adenosine receptor, exhibiting an IC50 value of 0.29 nM. It demonstrates a remarkable 14-fold selectivity towards the A2aR receptor in comparison to the A2bR receptor.