Hit-to-lead & Lead Optimization
Hits via screening or structure-based design are assessed for their chemical and biological properties. Our biology and chemistry teams progress promising compound series through hit-to-lead and lead-to-development candidate studies.
Our discovery biology team develops assays for a fully-integrated critical path that allows for testing compounds beyond the primary assay that can include selectivity and ortholog profiling. These assays are typically in low-volume 384-well format.
Our medicinal chemists have significant experience at pharmaceutical companies, biotech technology companies, and academia. We have solved the challenges of synthesizing and optimizing compounds across many different protein target classes and therapeutic indications including, CV disease, diabetes, infectious diseases, oncology, inflammation, CNS, and respiratory diseases. Our new laboratories are state-of-the-art with the highest standard of instrumentation. In addition, we employ world class computational chemistry to aid in our compound library designs and medicinal chemistry optimization programs.
We have established an in-house suite of in vitro ADME assays to determine drug-like properties including microsomal stability, protein binding, plasma stability, solubility, CYP450 binding, hERG binding & activity, cytotoxicity, and cell permeability.
Our in-house bioanalytical group collaborates with the discovery biology group to develop in vitro assays, and collaborates with our colleagues at Invivotek to study pharmacokinetic profiles of our lead compounds. Efficacy of lead compounds and PK/PD relationships are assessed using predictive in vivo models of disease.