All molecules

We are constantly expanding our molecule library.




We share an unprecedented, potent and selective orally bioavailable BCL6 degrader BI-1136 for collaborative research on novel disease indications. Partners would gain privileged access to our oral BCL6 degrader and collaborate with Boehringer Ingelheim scientists. Funding of up to €200.000 is available for each selected proposal. We invite scientists to submit proposals containing an in vivo testable hypothesis using our oral BCL6 degrader.


β2 adrenergic receptor (β2AR ) agonists have been used as bronchodilating agents for the last decades for the treatment of pulmonary diseases like asthma. BI-167107 was synthesized during a campaign to develop third generation of β2-agonists suitable for a once a day regimen. Due to its high potency and slow dissociation from the target it was subsequently used to support crystallization of active state β2AR and β2AR-G-protein complexes.

BI 1002494

BI 1002494 is due to its high potency, good physicochemical properties, suitable selectivity profile and low toxicity an excellent tool to explore SYK functions in vitro and in vivo.


With BI-0314 the first allosteric activator of tyrosine phosphatases is described. We hope to spark the design of selective allosteric ligands of phosphatases with the disclosure of the X-ray structure, and the elucidation of the mode of action of BI-0314 on STEP.


BI-1935 is a potent and selective small molecule inhibitor of Soluble epoxide hydrolase (sEH). In a biochemical binding assay h-sEH it shows an IC50 of 7 nM and is also highly active in a cellular Hep G2-DHET assay format (IC50 < 1 nM).


BI-2536 was the first potent and selective PLK1 inhibitor which entered clinical trials. It is a suitable in vitro and in vivo tool to study PLK function.


BI-9627 is a highly potent NHE1 inhibitor with low DDI potential, excellent pharmacokinetics, and good selectivity against NHE2 and NHE3.


BIII 890CL is a highly potent, selective and use-dependent voltage-dependent sodium channel blocker suitable for in vitro and in vivo biological experiments. The compound has a high selectivity for site 2 of the sodium channel and preferentially binds to the inactivated state of the channel with an IC50 of 77 nM based on patch clamp evaluations. In contrast, the binding at the resting state is only 18 µM.


BI-4394 is a potent and highly selective inhibitor of MMP-13 that can be used as tool compound to test biological hypotheses in vitro.

According to the UK Third Generation Cannabinoid Act, the molecule cannot be shipped to the United Kingdom.


BI-1950 potently inhibits the binding of LFA-1 to ICAM-1 with a KD value of 9 nM and the production of IL-2 in human PBMC and whole blood with an IC50 value of 3 nM and 120 nM, respectively.


BI-2540 is a potent inhibitor of HIV non-nucleoside reverse transcriptase (NNRT) and cross-reactive against clinically relevant mutants of reverse transcriptase. BI-2540 shows low clearance and good bioavailability upon p.o. dosing in rats. With BI-2439, a relatively close analog of BI-2540 with significantly lower activity (420-fold) is available as negative control for in vitro experiments.

HIV integrase
BI 224436

BI 224436 is the first non-catalytic-site integrase inhibitor (NCINI) reaching a clinical trial. It combines high solubility at all relevant physiological pH values with good cell permeability and good metabolic stability.


BI-1388 is a nanomolar to picomolar inhibitor of HCV NS3 protease activity and of viral replication for various HCV genotypes and for resistant mutants D168V and R155K.


BI-1230 is a single digit nanomolar inhibitor of HCV NS3 protease activity and of viral replication. BI-1230 was shown to be highly selective against other serine/cysteine proteases and to be suitable for in vivo studies.

BI 207127

BI 207127 (deleobuvir) is a highly potent inhibitor of the enzymatic function of NS5B, the RNA polymerase of HCV, and of viral replication  (~20 nM).


Our GSK-3 inhibitor BI-5521 with shown in vivo efficacy is characterized by high potency and good selecticvity.

BI 653048

BI 653048 is a “dissociated” GR agonist (displaying different transcriptional regulatory profiles between gene transrepression and transactivation) with selectivity for other nuclear receptors (MR, PR) and good drug-like properties.

BI 665915

BI 665915 demonstrates nanomolar FLAP binding potency and is a molecule suitable for testing biological hypotheses in vitro and also in vivo.

BI 99179

Our FAS in vivo tool compound BI 99179 is characterised by high potency, good selectivity and significant peripheral and central exposure upon oral administration in rats.


Chymase plays an important and diverse role in the homeostasis for a number of cardiovascular processes and has been linked to heart failure. BI-1942 is a potent inhibitor of human chymase with an IC50 value of 0.4 nM and >100 fold selectivity against Cathepsin G and is thus a suitable tool for testing biological hypotheses involving human Chymase in vitro.


BI-1347 is a selective nanomolar CDK8 inhibitor, suitable for testing biological hypotheses in vitro and also in vivo.


Our compound is the first small molecule inhibitor of the Chemokine receptor CCR10.1-3 It is a potent and selective compound and suitable for in vivo validation.

BI 639667

BI 639667 is a potent, selective human CCR1 antagonist with optimized drug-like properties.


BI-9740 is very potent, highly selective and orally bioavailable CatC inhibitor. BI-9740 shows no species selectivity and displays low nM IC50 in human, mouse and rat CatC assays. BI-9740 has high solubility at pH 2.2, 4.5 and 7. BI-9740 has very good in vitro and in vivo PK properties in several animal species (mouse, rat, mini pig).


BI-9564 binds with high affinity to BRD9 KD(BRD9, ITC) = 14 nM and with lower affinity to closely related BRD7 KD(BRD7, ITC) = 239 nM. CECR2 was the only other identified off-target (KD(CECR2, ITC) = 258 nM), but with no effect in cells at 1 µM (FRAP assay). BI-9464 is completely negative on BET family members in the AlphaScreen (>100 µM).


BI-7273 is a potent dual BRD7/BRD9 inhibitor with 30 fold better potency in the BRD7 AlphaScreen assay compared to our more selective BRD9 inhibitor BI-9564.

BET bromodomains
MZ 1

MZ 1 is a first in class l.m.w. degrader that tethers JQ1 to a VHL E3 ubiquitin ligase ligand, aimed at triggering the intracellular destruction of BET proteins. MZ 1 potently and rapidly induces reversible, long-lasting, and preferential removal of BRD4 over BRD2 and BRD3 in cells.


BI-3812 is a single digit nanomolar BCL6::Co-repressor inhibitor which also inhibits the BCL6::Co-repressor complex formation in cells (IC50 = 40 nM). BI-3812 is a classical PPI inhibitor probe compound for testing hypotheses around BCL6 biology in vitro.


BI-3802 is a single digit nanomolar BCL6::Co-repressor inhibitor which induces efficacious BCL6 protein degradation in several Diffuse large B-cell lymphoma (DLBCL) cell lines (e.g., DC50 = 20 nM in SU-DHL-4 cells).


BI-2545 inhibits human ATX with an IC50 of 2.2 nM. In human whole blood BI-2545 inhibits Autotaxin with an IC50 of 29 nM and in rat whole blood with an IC50 of 96 nM.

Aurora B
BI 831266

BI 831266 is a potent and selective Aurora B inhibitor that inhibits cell proliferation and could be used as tool compound testing biological hypotheses.


BI-4659 is a potent and selective inhibitor of Alk5 (IC50 = 19 nM) which effectively blocks cellular phosphorylation of Smad2/Smad3 in HaCaT cells (EC50 = 185 nM). We also offer BI-4101 as negative control. BI-4659 (5 mg) can be ordered free of charge together with BI-4101.1,6