All molecules

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-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.

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-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.

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

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.

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.

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-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 K_D(BRD9, ITC) = 14 nM and with lower affinity to closely related BRD7 K_D(BRD7, ITC) = 239 nM. CECR2 was the only other identified off-target (K_D(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-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 831266 is a potent and selective Aurora B inhibitor that inhibits cell proliferation and could be used as tool compound testing biological hypotheses.