Target identification

Identify important kinase drivers of disease

Applying deep expertise in computational and cell biology, we continually mine data and create pioneering disease models to gain insight into the biology of cancer and other debilitating diseases, and to identify new and promising kinase targets.

Genomics approach: Our high-capacity computing infrastructure enables us to rapidly analyze human tumor data using our proprietary algorithms.

Cell-based screens: A subset of compounds in our library exhibit remarkable potency and selectivity for particular kinases in disease-relevant, cell-based screens. Many of these compounds inhibit kinases of unknown biology, presenting an opportunity to evaluate their roles in human disease

Proprietary compound library

Isolate highly selective compounds as starting points

Our proprietary compound library is a unique, varied collection of small molecules, designed in-house as kinase inhibitors without specific kinases in mind. Annotating this library against the human kinome enables us to recognize starting points for medicinal chemistry, identify disease drivers, and efficiently select development candidates, yielding a diversity of novel chemical structures while refining our knowledge of the kinome. More than 450 kinases and disease-relevant kinase mutants are screened for selectivity and potency, and we relentlessly enhance our library with insights from our drug discovery research to spur future discovery.

Lead optimization

Optimize chemistry to target specifications

Our scientists apply in-depth medicinal chemistry expertise to design and optimize novel therapeutic candidates that can meet or exceed target profiles. From starting points generated by our compound library, we explore iterative medicinal chemistry optimization to improve potency, selectivity and pharmaceutical properties. In addition, our chemists use advanced structure-based design technologies, including crystallography and computer modeling.