Break New Ground in Drug Discovery with Paradigm-Shifting Chemistry

We pursue life-changing oral therapies by targeting disease drivers that have been difficult-to-drug with existing chemistry. Our approach transforms dormant carbon-hydrogen (C-H) bonds – the most common bonds in small molecules – into powerful building blocks of novel drug architectures. With unprecedented speed and precision, we can finally create extraordinary diversity in coveted chemical space to unlock first- and best-in-class therapies.

Innovative Medicines Demand Chemistry Innovation

Medicinal chemists have relied heavily on a handful of reactions since the 1990s. This has limited the industry to explore only a small fraction of the 3D chemical space. Novel, diverse molecular architectures are highly desired for addressing tough targets or mechanisms such as modulating protein-protein interactions, but they have been difficult to access at scale. Until now.

Edit C-H Bonds with Atomic-level Precision

At Architect, we exploit transformative chemistry known as C-H bond activation to create unprecedented diversity of 3D drug molecules previously out of reach.

C-H bonds are the most common bonds in small molecules, yet they are notoriously difficult to modify. Leveraging decades of breakthroughs from our founder, Jin-Quan Yu, we can edit these bonds with unmatched breadth, speed, and selectivity to rapidly discover and progress innovative medicines.

“Jin-Quan Yu’s unconventional approach to C-H functionalization is creating a paradigm shift in the logic of synthetic chemistry and breaking down barriers to the development of versatile compounds with enormous benefits to academic, industrial, and pharmaceutical research.”

Integrated Discovery Engine Maximizes Success of Covalent & Non-Covalent Drug Discovery

Our platform integrates both covalent and non-covalent approaches to rapidly identify and progress high-quality starting points for broad classes of challenging targets. We apply C-H activation to design and synthesize novel 3D scaffolds, which feed our proprietary libraries and advanced screening platforms (DEL, nano-scale synthesis, chemical proteomics).

Our pipeline focuses on chemically challenging, biologically validated targets. We aim to pursue first- and best-in-class therapies, with an emphasis in immunology and oncology, but our platform can be applied to any disease area.

Architect Novel 3D Cores platform