List of works - Jim Nonomiya

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

scientific article published on 23 July 2013

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: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

scientific article published on 07 January 2019

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

scientific article

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

scientific article

Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor

scientific article

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

scientific article

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 Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition ⬇️

scientific article published on June 11, 2012

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

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 a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling

scientific article published on 04 April 2019

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization

scientific article

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

scientific article

Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors

scientific article

GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway

scientific article published on 13 October 2011

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity

scientific article published on 29 June 2013

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

scientific article published on 12 March 2010

Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.

scientific article published in March 2007

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy

scientific article published in April 2008

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta

scientific article

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf ⬇️

scientific article published on May 17, 2012

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

scientific article published on 15 April 2011

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

scientific article published on 12 December 2012

Preclinical Characterization of PF-00868554, a Potent Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

scientific article (publication date: June 2009)

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

scientific article

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

Structure of the catalytic domain of human polo-like kinase 1

scientific article

Structure of the catalytic domain of human protein kinase C beta II complexed with a bisindolylmaleimide inhibitor

scientific article

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis

scientific article published on 29 June 2015

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

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

scientific article published on 11 September 2012

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

scientific article

List of works by Jim Nonomiya

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

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: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor

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

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 Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition ⬇️

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

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 a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization

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

Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors

GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity

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

Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf ⬇️

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Preclinical Characterization of PF-00868554, a Potent Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

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

Structure of the catalytic domain of human polo-like kinase 1

Structure of the catalytic domain of human protein kinase C beta II complexed with a bisindolylmaleimide inhibitor

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis

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

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

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

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.