List of works - Timothy P Heffron

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

scientific article

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

scientific article published on 24 February 2015

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

scientific article

CNS Anticancer Drug Discovery and Development Conference White Paper.

scientific article

CNS Anticancer Drug Discovery and Development: 2016 conference insights

scientific article published on 18 July 2017

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

scientific article published on 16 September 2017

Characterization of Anti-Neovascularization Activity and Ocular Pharmacokinetics of PI3K/mTOR Inhibitor GNE-947

scientific article published on 04 March 2020

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

scientific article

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

scientific article published on 11 March 2016

DEGAS: Sharing and Tracking Target Compound Ideas with External Collaborators ⬇️

scientific article published on November 28, 2011

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

scientific article published on 26 June 2019

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 ro

scientific article published on 3 June 2013

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

scientific article published on 16 February 2016

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

scientific article

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 ⬇️

scientific article published on October 7, 2011

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

scientific article

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

scientific article published on 15 January 2014

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

scientific article

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

scientific article

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

scientific article published on 29 November 2018

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

scientific article published on 12 March 2010

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

scientific article published on April 2010

Ladder polyether synthesis via epoxide-opening cascades using a disappearing directing group

scientific article

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

scientific article

Noncovalent wild-type-sparing inhibitors of EGFR T790M

scientific article published on 10 December 2012

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

scientific article

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

scientific article published on 17 December 2015

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform ⬇️

scientific article published on October 21, 2011

SiMe3-based homologation-epoxidation-cyclization strategy for ladder THP synthesis

scientific article published on 01 June 2003

Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer

scientific article

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase ⬇️

scientific article published on May 13, 2011

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

scientific article published on August 19, 2010

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

scientific article

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

scientific article published on 11 September 2012

List of works by Timothy P Heffron

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

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

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

CNS Anticancer Drug Discovery and Development Conference White Paper.

CNS Anticancer Drug Discovery and Development: 2016 conference insights

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

Characterization of Anti-Neovascularization Activity and Ocular Pharmacokinetics of PI3K/mTOR Inhibitor GNE-947

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

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

DEGAS: Sharing and Tracking Target Compound Ideas with External Collaborators ⬇️

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

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 ro

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

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

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 ⬇️

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

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

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

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

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

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

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

Ladder polyether synthesis via epoxide-opening cascades using a disappearing directing group

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

Noncovalent wild-type-sparing inhibitors of EGFR T790M

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

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

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform ⬇️

SiMe3-based homologation-epoxidation-cyclization strategy for ladder THP synthesis

Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase ⬇️

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

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

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