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).

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

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-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-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.