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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.
MZ1 is a first in class PROTAC (proteolysis-targeting chimeras) that tethers JQ1 to a VHL E3 ubiquitin ligase ligand, aimed at triggering the intracellular destruction of BET proteins.
With BI-0314 the first allosteric activator of tyrosine phosphatases is described. We hope to spark the design of selective allosteric ligands of phosphatases with the disclosure of the X-ray structure, and the elucidation of the mode of action of BI-0314 on STEP.
BI-5521 is a potent and selective ATP-competitive small molecule inhibitor of glycogen synthase kinase 3 (GSK-3) with demonstrated in vivo activity. The N-alkylated derivative BI-4481 is also available as negative control.
Chymase plays an important and diverse role in the homeostasis for a number of cardiovascular processes and has been linked to heart failure.