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BI-0474
BI-0474 is a selective and potent irreversible covalent KRASG12C 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.
BI-5121
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.
BI-1030
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
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
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.
BI-8255
Gram-positive bacteria and mycobacteria utilize a protein degradation system, ClpCP, which acts analogous to the eukaryotic ubiquitin protein degradation machinery. With BI-8255 that represents a proof-of-concept compound targeting BRDT, we have established a versatile research tool enabling the inducible degradation of bacterial proteins …
BI-8128
BI-8128 is a reversible and highly selective, fourth generation EGFR inhibitor suitable for in vitro and in vivo studies with potent activity against the primary oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.
BI-3434
BI-3434 is a potent peptidic secretin receptor (SctR) agonist that serves as a high-quality in vitro and in vivo tool compound. The agonist shows high potency with good selectivity and a prolonged half-life in mice.
BI 894999
BI 894999 is a small molecule oral BET inhibitor suitable for in vitro and in vivo studies. BET family proteins are key regulators of transcription. The related molecule BI-6953 is available as a negative control.
BI-9593
BI-9593 is a potent and selective orally bioavailable PHGDH inhibitor. Its high permeability and tolerability render it ideal for in vivo as well as cellular profiling. Its stereoisomer BI-9594 is available as negative control.
BI-1136
With BI-1136, we share an unprecedented, selective orally bioavailable BCL6 degrader with nanomolar potency. The molecule is suitable for in vivo testing in rodents and displays good tolerability. Mechanistically, the molecule acts as a BCL6-specific protein degrader and induces strong expression of BCL6-repressed genes.
BI-3231
BI-3231 is potent and selective inhibitor of hydroxysteroid 17-beta dehydrogenase 13 (HSD17B13), a lipid droplet-associated enzyme primarily expressed in hepatocytes and whose exact function and substrates are unknown. BI-3231 is selective over other HSD17B family members and has been extensively characterized both in vitro and in vivo.