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OX1
BI-5121
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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.

GABAA α5
BI-1030
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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 …

GPR88
BI-9508
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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.

TPP
BI-5232
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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.

BacPROTAC
BI-8255
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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 …

EGFR
BI-8128
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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.

SctR
BI-3434
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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.

BET
BI 894999
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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.