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Orexins are potent neuropeptides interacting with G protein-coupled receptors known as orexin type-1 and type-2 receptors. BI-5121 is a selective orexin type 1 receptor antagonist with high in vitro potency. Furthermore, BI-5121 has been shown to be efficacious in vivo in the behavioral 5-choice serial reaction time task in Lister Hooded rats.

GABA type A receptors are chloride ion channels that drive inhibitory neurotransmission in the mammalian central nervous system upon binding of GABA, the primary inhibitory neurotransmitter in the central nervous system. BI-1030 is one of the few molecules in the literature are showing subtype selectivity for the GABAA receptors …

BI-9508 is a potent and selective agonist of the G-protein-coupled receptor 88 (GPR88). It displays improved brain penetration properties compared to earlier agonists. The closely related compound BI-0823 is available as a negative control.

BI-5232 is a drug-like non-natural ligand of the thiM aptamer of the TPP riboswitch with potencies near equal to TPP itself. It has been shown to cellularly induce transgene expression in constructs using both the native aptamer as well as a site-directed mutant which does not bind TPP.