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.

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-1950 potently inhibits the binding of LFA-1 to ICAM-1 with a K_D 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 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-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 665915 demonstrates nanomolar FLAP binding potency and is a molecule suitable for testing biological hypotheses in vitro and also in vivo.

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-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.

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-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.