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

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.

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-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-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.