Genentech: Tim Heffron | Associate Director, Principal Scientist, Discovery Chemistry

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Scientists / Our Scientists

"Each day we work to extend and improve lives."

14

Years at Genentech

32

Publications

I joined the Discovery Chemistry department at Genentech as a Medicinal Chemist in 2005 after completing my PhD in organic chemistry at MIT. I now lead interdisciplinary teams focused on the discovery of new drugs to extend and improve people’s lives.

Featured Publication

As a chemist, my work can focus on designing drugs directed to whatever target is most compelling from a biological point of view without being confined to a particular therapeutic area. In my time at Genentech I have contributed to programs directed toward the discovery of new therapeutics for oncology (including cancer immunotherapy), neuro-oncology, neurology, and ophthalmology indications. Each program brings unique scientific challenges and a need to innovate to discover new medicines.

Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer

Structure,

Ping Wu; Christopher J. Sneeringer; Keith E. Pitts; Eric S. Day; Bryan Chan; Binqing Wei; Isabelle Lehoux; Kyle Mortara; Hong Li; Jiansheng Wu; Yvonne Franke; John Moffat; Jane Grogan; Tim Heffron; Weiru Wang

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Sarah M. Bronner; Karl A. Merrick; Jeremy Murray; Laurent Salphati; John Moffat; Jodie Pang; Christopher Sneeringer; Nick Dompe; Patrick Cyr; Hans Purkey; Gladys de Leon Boenig; Jun Li; Aleksandr Kolesnikov; Larouche-Gauthier; Kwong Wah Lai; Xiaoli Shen; Samuel Aubert-Nicol; Yi-Chen Chen; Jonathan Cheong; James Crawford; Marc Hafner; Pouyan Haghshenas; Araz Jakalian; Jean-Philippe Leclerc; Ngiap-Kie Lim; Thomas O'Brien; Emile Plise; Shalan; Claudio Sturino; John Wai; Yang Xiao; Peter Yin; Zhao; Stephen Gould; Alan Olivero; Tim Heffron

Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels

Neuro-Oncology, ISSN: 15235866 15228517

Tim Heffron

Brain distribution and efficacy of the brain penetrant PI3K inhibitor GDC-0084 in orthotopic mouse models of human glioblastoma

Drug Metabolism and Disposition, ISSN: 1521009X

Laurent Salphati; Bruno Alicke; Tim Heffron; Sheerin Latham; Merry Nishimura; Cao; Rick Carano; Jonathan Cheong; Joan Greve; Hartmut Koeppen; Shari Lau; Leslie Lee; Michelle Nannini; Jodie Pang; Emile Plise; Cristine Quiason; Linda Rangell; Xiaolin Zhang; Stephen Gould; Heidi Phillips; Alan Olivero

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Journal of Medicinal Chemistry, ISSN: 15204804

Bryan Chan; Emily Hanan; Krista Bowman; Callie Bryan; Dan Burdick; Emily Chan; Yuan Chen; Saundra Clausen; Trisha Dela Vega; Jenna Dotson; Charles Eigenbrot; Richard Elliott; Robert Heald; Philip Jackson; Jamie D. Knight; Hank La; Michael Lainchbury; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen M. Seward; Steve Sideris; Lily Shao; Shumei Wang; Siew Kuen Yeap; Ivana Yen; Christine Yu; Tim Heffron

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

ACS Medicinal Chemistry Letters, ISSN: 19485875

Tim Heffron; Chudi Ndubaku; Laurent Salphati; Bruno Alicke; Jonathan Cheong; Joy Drobnick; Kyle Edgar; Stephen Gould; Leslie Lee; John Lesnick; Cris Lewis; Jim Nonomiya; Jodie Pang; Emile Plise; Steve Sideris; Jeffrey Wallin; Lan Wang; Xiaolin Zhang; Alan Olivero

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Journal of Medicinal Chemistry, ISSN: 15204804

Tim Heffron; Robert Heald; Chudi Ndubaku; Binqing Wei; Martin Augistin; Steven Do; Kyle Edgar; Charles Eigenbrot; Lori Friedman; Emanuela Gancia; Philip Jackson; Graham Jones; Aleksandr Kolesnikov; Leslie B. Lee; John Lesnick; Cris Lewis; Neville J. McLean; Mario Mörtl; Jim Nonomiya; Jodie Pang; Steve Price; Wei Wei Prior; Laurent Salphati; Steve Sideris; Steven Staben; Stefan Steinbacher; Vickie Tsui; Jeffrey Wallin; Deepak Sampath; Alan Olivero

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 14643405

Emily Hanan; Matt Baumgardner; Callie Bryan; Yuan Chen; Charles Eigenbrot; Peter Fan; Xiao-Hui Gu; Hank La; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Steve Sideris; Ivana Yen; Christine Yu; Tim Heffron

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR

ACS Medicinal Chemistry Letters, ISSN: 19485875

Callie Bryan; Dan Burdick; Bryan Chan; Yuan Chen; Saundra Clausen; Jenna Dotson; Charles Eigenbrot; Richard Elliott; Emily Hanan; Robert Heald; Philip Jackson; Hank La; Michael Lainchbury; Shiva Malek; Sam E. Mann; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen Seward; Steve Sideris; Shumei Wang; Ivana Yen; Christine Yu; Tim Heffron

The Discovery and Process Chemistry Development of GDC-0084, a Brain Penetrating Inhibitor of PI3K and mTOR

ACS Symposium Series, ISSN: 19475918

Tim Heffron; Andrew McClory; Andy Stumpf

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Journal of Medicinal Chemistry, ISSN: 15204804

Robert Heald; Krista Bowman; Callie Bryan; Dan Burdick; Bryan Chan; Emily Chan; Yuan Chen; Saundra Clausen; Belen Dominguez-Fernandez; Charles Eigenbrot; Richard Elliott; Emily Hanan; Philip Jackson; Jamie Knight; Hank La; Michael Lainchbury; Shiva Malek; Sam E. Mann; Mark Merchant; Kyle Mortara; Hans Purkey; Gabriele Schaefer; Stephen Schmidt; Eileen Seward; Steve Sideris; Lily Shao; Shumei Wang; Kuen Yeap; Ivana Yen; Christine Yu; Tim Heffron

A probabilistic method to report predictions from a human liver microsomes stability QSAR model: A practical tool for drug discovery

Journal of Computer-Aided Molecular Design, ISSN: 15734951

Ignacio Aliagas; Alberto Gobbi; Tim Heffron; Man Ling Lee; Dan Ortwine; Mark Zak; Cyrus Khojasteh

CNS Anticancer Drug Discovery and Development Conference White Paper

Neuro-Oncology, ISSN: 15235866

Victor A. Levin; Peter J. Tonge; James M. Gallo; Marc R. Birtwistle; Arvin C. Dar; Antonio Iavarone; Patrick J. Paddison; Tim Heffron; William F. Elmquist; Jean E. Lachowicz; Ted W. Johnson; Forest M. White; Joohee Sul; Smith; Wang Shen; Jann N. Sarkaria; Ramakrishna Samala; Patrick Y. Wen; Donald A. Berry; Russell C. Petter

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Journal of Medicinal Chemistry, ISSN: 15204804

Emily Hanan; Charles Eigenbrot; Callie Bryan; Dan Burdick; Bryan Chan; Yuan Chen; Jenna Dotson; Robert Heald; Philip Jackson; Hank La; Michael Lainchbury; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen M. Seward; Steve Sideris; Christine Tam; Shumei Wang; Siew Kuen Yeap; Ivana Yen; Peter Yin; Christine Yu; Inna Zilberleyb; Tim Heffron

Discovery of highly potent, selective, and brain-penetrant aminopyrazole Leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

Journal of Medicinal Chemistry, ISSN: 15204804

Tony Estrada; Bryan Chan; Charles Baker-Glenn; Alan Beresford; Dan Burdick; Mark Chambers; Huifen Chen; Sara Dominguez; Jenna Dotson; Jake Drummond; Mike Flagella; Reina Fuji; Andrew Gill; Jason Halladay; Seth Harris; Tim Heffron; Tracy Kleinheinz; Donna Lee; Claire Le Pichon; Xingrong Liu; Joe Lyssikatos; Andrew D. Medhurst; John Moffat; Kevin Nash; Kimberly Scearce-Levie; Zejuan Sheng; Daniel Shore; Susan Wong; Shuo Zhang; Xiaolin Zhang; Haitao Zhu; Zach Sweeney

Prevalence of acid-reducing agents (ARA) in cancer populations and ARA drug-drug interaction potential for molecular targeted agents in clinical development

Molecular Pharmaceutics, ISSN: 15438384

Gillian S. Smelick; Tim Heffron; Laura Chu; Brian Dean; David West; Scott L. Duvall; Bert Lum; Nageshwar Budha; Scott Holden; Leslie Z. Benet; Adam Frymoyer; Mark Dresser; Joseph Ware

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d ][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2- methylpropanamide (GDC-0032): A β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity

Journal of Medicinal Chemistry, ISSN: 00222623

Chudi Ndubaku; Tim Heffron; Steven Staben; Matt Baumgardner; Nicole Blaquiere; Erin Bradley; Richard J. Bull; Steven Do; Jenna Dotson; Danette Dudley; Kyle Edgar; Lori Friedman; Rich Goldsmith; Robert Heald; Aleksandr Kolesnikov; Leslie Lee; Cris Lewis; Michelle Nannini; Jim Nonomiya; Jodie Pang; Steve Price; Wei Wei Prior; Laurent Salphati; Steve Sideris; Jeffrey Wallin; Lan Wang; Binqing Wei; Deepak Sampath; Alan Olivero

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Chudi Ndubaku; Nicole Blaquiere; Marcia Belvin; Richard J. Bull; Danette Dudley; Kyle Edgar; Daniel Gray; Robert Heald; Tim Heffron; Graham E. Jones; Mark Jones; Aleksandr Kolesnikov; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Neville J. McLean; Jim Nonomiya; Alan Olivero; Rachel Ord; Jodie Pang; Stephen Price; Wei Wei Prior; Lionel Rouge; Laurent Salphati; Deepak Sampath; Jeffrey Wallin; Lan Wang; Binqing Wei; Christian Weismann; Ping Wu

Noncovalent wild-type-sparing inhibitors of EGFR T790M

Cancer Discovery, ISSN: 21598274

Ho-June Lee; Gabriele Schaefer; Tim Heffron; Lily Shao; Xiaofen Ye; Steve Sideris; Shiva Malek; Emily Chan; Mark Merchant; Hank La; Savita Ubhayakar; Bob Yauch; Valentina Pirazzoli; Katerina Politi; Jeffrey Settleman

Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Nicole Blaquiere; Vickie Tsui; Aleksandr Kolesnikov; Steven Do; Erin Bradley; Jenna Dotson; Rich Goldsmith; Tim Heffron; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Alan Olivero; Jodie Pang; Lionel Rouge; Laurent Salphati; Binqing Wei; Christian Wiesmann; Ping Wu

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

Journal of Medicinal Chemistry, ISSN: 00222623

Tony Estrada; Xingrong Liu; Charles Baker-Glenn; Alan Beresford; Dan Burdick; Mark Chambers; Bryan Chan; Huifen Chen; Xiao Ding; Antonio DiPasquale; Sara Dominguez; Jenna Dotson; Jake Drummond; Mike Flagella; Sean Flynn; Reina Fuji; Andrew Gill; Janet Gunzner-Toste; Seth Harris; Tim Heffron; Tracy Kleinheinz; Donna Lee; Claire Le Pichon; Joe Lyssikatos; Andrew D. Medhurst; John Moffat; Susmith Mukund; Kevin Nash; Kimberly Scearce-Levie; Zejuan Sheng; Daniel Shore; Thuy Tran; Naimisha Trivedi; Shumei Wang; Shuo Zhang; Xiaolin Zhang; Guiling Zhao; Haitao Zhu; Zach Sweeney

Targeting the PI3K pathway in the brain - Efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

Clinical Cancer Research, ISSN: 10780432

Laurent Salphati; Tim Heffron; Bruno Alicke; Merry Nishimura; Kai Barck; Rick Carano; Jonathan Cheong; Kyle Edgar; Joan Greve; Samir Kharbanda; Hartmut Koeppen; Shari Lau; Leslie Lee; Jodie Pang; Emile Plise; Jenny L. Pokorny; Hani Bou-Reslan; Jann N. Sarkaria; Jeffrey Wallin; Xiaolin Zhang; Stephen Gould; Alan Olivero; Heidi Phillips

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α

Journal of Medicinal Chemistry, ISSN: 00222623

Tim Heffron; Laurent Salphati; Bruno Alicke; Jonathan Cheong; Jenna Dotson; Kyle Edgar; Rich Goldsmith; Stephen Gould; Leslie Lee; John Lesnick; Cris Lewis; Chudi Ndubaku; Jim Nonomiya; Alan Olivero; Jodie Pang; Emile Plise; Steve Sideris; Sean Trapp; Jeffrey Wallin; Lan Wang; Xiaolin Zhang

DEGAS: Sharing and tracking target compound ideas with external collaborators

Journal of Chemical Information and Modeling, ISSN: 15205142

Man Ling Lee; Ignacio Aliagas; Jenna Dotson; JW Feng; Alberto Gobbi; Tim Heffron

Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform

Journal of Medicinal Chemistry, ISSN: 00222623

Tim Heffron; Binqing Wei; Alan Olivero; Steven Staben; Vickie Tsui; Steven Do; Jenna Dotson; Adrian J. Folkes; Paul Goldsmith; Rich Goldsmith; Janet Gunzner-Toste; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Stephen Shuttleworth; Dan Sutherlin; Nan Chi Wan; Shumei Wang; Christian Wiesmann; Bing-Yan Zhu

Discovery of a potent, selective, and orally available class i phosphatidylinositol 3-kinase (PI3K)/Mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer

Journal of Medicinal Chemistry, ISSN: 00222623

Dan Sutherlin; Linda Bao; Megan Berry Swadell; Georgette Castanedo; Irina Chuckowree; Jenna Dotson; Adrian Folks; Lori Friedman; Rich Goldsmith; Janet Gunzner-Toste; Tim Heffron; John Lesnick; Cris Lewis; Simon Mathieu; Jeremy Murray; Jim Nonomiya; Jodie Pang; Neil Pegg; Wei Wei Prior; Lionel Rouge; Laurent Salphati; Deepak Sampath; Qingping Tian; Vickie Tsui; Nan Chi Wan; Shumei Wang; Binqing Wei; Christian Wiesmann; Ping Wu; Bing-Yan Zhu; Alan Olivero

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Mike Siu; Rich Goldsmith; Alan Olivero; Steven Do; Dan Burdick; Tim Heffron; Jenna Dotson; Dan Sutherlin; Bing-Yan Zhu; Vickie Tsui; Hoa Le; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Jodie Pang; Wei Wei Prior; Laurent Salphati; Lionel Rouge; Deepak Sampath; Steve Sideris; Christian Wiesmann; Ping Wu

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Tim Heffron; Dan Sutherlin; Seema Bhat; Georgette Castanedo; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Lori Friedman; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Alan Olivero; Emile Plise; Jodie Pang; Wei Wei Prior; Laurent Salphati; Lionel Rouge; Deepak Sampath; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Weismann; Ping Wu; Bing-Yan Zhu

Ladder polyether synthesis via epoxide-opening cascades directed by a disappearing trimethylsilyl group

Journal of Organic Chemistry, ISSN: 00223263

Tim Heffron; Graham L. Simpson; Estibaliz Merino; Timothy F. Jamison

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Tim Heffron; Megan Berry Swadell; Georgette Castanedo; Christine Chang; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Janet Gunzner-Toste; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; David Peterson; Laurent Salphati; Deepak Sampath; Steve Sideris; Dan Sutherlin; Vickie Tsui; Nan Chi Wan; Shumei Wang; Susan Wong; Bing-Yan Zhu

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available Pan-PI3-kinase and dual Pan-PI3-kinase/mTOR inhibitors for the treatment of cancer

Journal of Medicinal Chemistry, ISSN: 00222623

Dan Sutherlin; Deepak Sampath; Megan Berry Swadell; Georgette Castanedo; Zhigang Chang; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Lori Friedman; Rich Goldsmith; Tim Heffron; Leslie Lee; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; Wei Wei Prior; Laurent Salphati; Steve Sideris; Qingping Tian; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Wiesmann; Susan Wong; Bing-Yan Zhu

Concerning Lewis acid promoted, directing-group-free epoxide-ring-opening cascades

Synlett, ISSN: 09365214

Tim Heffron; Timothy F. Jamison

Massachusetts Institute of Technology, Organic Chemistry, Ph. D. – 2005
Yale University, Chemistry, B.S. – 2000