On September 14, 2016 – Third Rock Ventures, LLC reported the formation
of Relay Therapeutics with $57 million in Series A financing, including participation from an affiliate of
D. E. Shaw Research, LLC (Press release, Relay Therapeutics, SEP 14, 2016, View Source [SID1234520734]).

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Relay Therapeutics is building the world’s first dedicated drug discovery
platform centered on protein motion, with the aim of designing and developing new medicines that will
make a transformative difference for patients. Relay’s novel approach will build on recent scientific and
technological advances in structural biology, biophysics, computation, chemistry and biology to create
an integrated drug discovery engine fueled by a detailed understanding of the dynamic structural
changes undergone by protein molecules within the body. The company’s groundbreaking activities are
being spearheaded by a team that includes some of the world’s leaders in these emerging areas.
"Our integration of protein motion into the heart of the drug discovery process represents both a
philosophical and technological once-in-a-generation paradigm shift," said Alexis Borisy, Executive
Chairman and interim CEO of Relay Therapeutics, and Partner at Third Rock Ventures. "At Relay, we
have assembled the team and tools to build the first company with a dedicated drug discovery pipeline
centered around protein motion. This advancement in drug discovery – from static to dynamic – creates
opportunities to develop more effective therapies that we believe will improve and extend the lives of
millions of patients."

Scientific Approach
While much of biology is controlled by the three-dimensional motion of proteins, this reality is not
reflected in today’s drug discovery process. Relay Therapeutics is using emerging technologies and
insights to move from a static perspective to a moving one, allowing for the rational discovery and
design of medicines for diseases where effective therapies do not currently exist. The company’s drug
discovery engine illuminates the full mobility of a protein and the ways in which protein motion
regulates function. By applying these technologies as an integrated team focused on disease-causing
targets, Relay Therapeutics aims to develop breakthrough medicines for patients in need. The
company’s initial programs are focused on oncology.
"Relay’s novel approach enables us to observe large-scale and subtle protein motions, identifying new
opportunities for the drug design process," said Mark Murcko, Ph.D., Chief Scientific Officer of Relay
Therapeutics. "This innovative and integrated approach allows us to pursue novel medicines against a
wide array of compelling drug targets that, until now, have been challenging or even inaccessible."
History of Protein Motion in Drug Discovery
Sixty years ago, scientists acquired the ability to generate detailed static images of the molecular
machines that operate within our bodies, yielding an improved understanding of the molecular
underpinnings of certain diseases. By the late 1980s, after a generation of technological improvements,
the adoption of these stationary molecular snapshots into the drug discovery process marked a turning
point in the history of the pharmaceutical industry, accelerating the design of more effective drugs. In
recent years, however, it has become clear that such static images tell only part of the story, and that the
emerging ability to observe how these machines move, function, and interact has the potential to once
again transform the process of drug design. Today – two generations after the first static pictures of
molecular structures, and one generation after they were first incorporated into drug discovery – Relay
Therapeutics is drawing on new computational and experimental advances to move beyond the era of
static snapshots into one in which movies of the body’s molecular machines become central to drug
discovery.
Founders
Relay Therapeutics was founded by a group of experts in structural biology, biophysics and
biomolecular simulation who have played a pioneering role in the development of technologies that are
central to the company’s approach. The founding team is applying this expertise to Relay’s drug
discovery efforts, focusing on achieving a deeper understanding of the relationship between protein
motion and drug action. The company founders are:
• Matthew Jacobson, Ph.D., Professor and Pharmaceutical Chemistry Department Chair,
University of California, San Francisco (UCSF)
• Dorothee Kern, Ph.D., Professor, Brandeis University; Investigator, Howard Hughes Medical
Institute
• Mark Murcko, Ph.D., Chief Scientific Officer and Co-Founder, Relay Therapeutics; Senior
Lecturer, Massachusetts Institute of Technology (MIT)
• D. E. Shaw Research (David E. Shaw, Ph.D., Chief Scientist)
About Relay Therapeutics
Relay Therapeutics is committed to discovering and developing medicines that will make a
transformative difference for patients by building the first dedicated drug discovery pipeline centered on
protein motion. Bringing together the latest scientific advances in structural biology, biophysics,
computation, chemistry and biology, Relay’s drug discovery engine illuminates the full mobility of a
protein and the ways in which protein motion regulates function. By applying this approach as an
integrated team focused on disease-causing targets, Relay aims to develop breakthrough medicines for
patients in need. The company’s initial programs are focused on developing therapeutics in oncology.
Headquartered in Cambridge, Massachusetts, Relay Therapeutics is a private company launched in 2016
with $57 million in Series A financing from Third Rock Ventures and an affiliate of D. E. Shaw
Research.