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AXPSP0056 is a selective allosteric GCH1 inhibitor that acts as a mimic of tetrahydrobiopterin (BH4). By occupying the latter’s binding site on GCH1, it triggers a feedback inhibition mechanism that decreases GCH1’s activity in the presence of elevated cellular concentrations of BH4. It is a single digit micromolar inhibitor.

BI-0474 is a selective and potent irreversible covalent KRAS^G12C inhibitor, developed using an NMR-based fragment screening approach pioneered at Vanderbilt University, whereby small molecules that bind reversibly to the KRAS switch II pocket were identified and optimized using structure-based design, and then a covalent “warhead” was attached.

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 …