All molecules

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.

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).

We believe that BI-0319 is a valuable tool to effectively reduce PTK2 protein levels in cell lines to reveal and differentiate between kinase- dependent and -independent functions of PTK2.

BIII 277CL is a selective high affinity blocker of the NMDA receptor ion channel (K_i = 4.5 nM), which displayed beneficial effects in reducing the cortical infarct area in mice with focal cerebral ischemia.
We offer BIII 277CL to test biological hypotheses in vitro and in vivo.

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-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.