Constellation has established an integrated set of technologies consisting of target validation tools, biochemical, biophysical, and cell-based assays, as well as preferred compound collections against targets in each of the writer, eraser, and reader classes. Our knowledge of these classes serves as the foundation for a powerful drug discovery platform. This deep know-how, together with our integrated suite of tools, serves as our product engine, which we deploy across all stages of the drug discovery process to commence advance new programs rapidly.
Target Selection/Functional Validation
Constellation has built industry-leading expertise in the development and application of reagents and tools that uncover the activity of epigenetic targets in disease. This includes the use of bioinformatics tools, chemical probe compounds and customized RNAi libraries. Constellation deploys these tools in biologically relevant and clinically validated models of cancer and inflammation to identify novel epigenetic targets with functional validation.
Constellation has developed a suite of biochemical assays that are used for high throughput screening as well as selectivity panels. Substrates range from simple histone peptides to complex oligonucleosomes with pre-installed chemical modifications. Constellation rigorously selects assay formats that recapitulate the most biologically relevant context, allowing us to identify inhibitors with the greatest potential.
Constellation has developed a collection of cell-based assays that assess the mechanism of action of our inhibitors as well as determine their phenotypic effects on a variety of cell types including but not restricted to cancer cells and immune cells. As a result, we have the ability to connect the on-target activity of our inhibitors directly to their disease-modifying effects.
High Throughput Screening & Hit Validation
Constellation has built a state-of-the-art, automated high throughput screening facility that is used routinely to screen our compound and RNAi libraries against epigenetic targets. Constellation has also developed a full range of biophysical assays to validate compounds as true inhibitors of targets of interest. Through these efforts, Constellation has created focused libraries that bind to targets in the writer, eraser, and reader families.
Structural biology is a core element of Constellation’s drug discovery platform. We have solved novel structures of targets and multiple co-crystals with our inhibitors to help guide our rational design efforts.
Constellation uses a variety of tools, including gene expression analysis, ChIP-chip, ChIP-Seq and tissue profiling, to identify biomarkers that will be used to select patient populations that will benefit the most from treatment with our therapies.