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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8762-8782

2015

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Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.419-432

2015

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Evaluating the Differences in Cycloalkyl Ether Metabolism Using the Design Parameter “Lipophilic Metabolism Efficiency” (LipMetE) and a Matched Molecular Pairs Analysis

Journal of medicinal chemistry, 2013-09, Vol.56 (17), p.6985-6990

2013

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Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes

ACS chemical neuroscience, 2010-06, Vol.1 (6), p.420-434

2010

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Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy

Journal of medicinal chemistry, 2009-12, Vol.52 (24), p.7946-7949

2009

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Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery

ACS chemical neuroscience, 2016-06, Vol.7 (6), p.767-775

2016

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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging

Journal of medicinal chemistry, 2017-10, Vol.60 (20), p.8538-8551

2017

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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor

Journal of medicinal chemistry, 2017-07, Vol.60 (13), p.5673-5698

2017

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Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties

ACS chemical neuroscience, 2010-06, Vol.1 (6), p.435-449

2010

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Total Synthesis of (+)-Phorboxazole A Exploiting the Petasis−Ferrier Rearrangement

Journal of the American Chemical Society, 2001-11, Vol.123 (44), p.10942-10953

2001

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Quantitative Assessment of the Impact of Fluorine Substitution on P‑Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability

Journal of medicinal chemistry, 2016-06, Vol.59 (11), p.5284-5296

2016

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Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

ACS medicinal chemistry letters, 2012-03, Vol.3 (3), p.187-192

2012

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Strategies to optimize the brain availability of central nervous system drug candidates

Expert opinion on drug discovery, 2011-04, Vol.6 (4), p.371-381

2011

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Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4568-4579

2013

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Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia

Journal of medicinal chemistry, 2009-08, Vol.52 (16), p.5188-5196

2009

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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19

Journal of medicinal chemistry, 2024-04

2024

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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE

Cell chemical biology, 2021-02, Vol.28 (2), p.148-157.e7

2021

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Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK

The Journal of pharmacology and experimental therapeutics, 2016-02, Vol.356 (2), p.410

2016

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Design and Discovery of 6‑[(3S,4S)‑4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro‑2H‑pyran-4-yl)-1,5-dihydro‑4H‑pyrazolo[3,4‑d]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9045-9054

2012

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An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

Science (American Association for the Advancement of Science), 2021-12, Vol.374 (6575), p.1586-1593

2021

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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.1001-1018

2018

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Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.861-877

2014

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Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo

The Journal of pharmacology and experimental therapeutics, 2012-05, Vol.341 (2), p.396

2012

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Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9055-9068

2012

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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway

Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

Evaluating the Differences in Cycloalkyl Ether Metabolism Using the Design Parameter “Lipophilic Metabolism Efficiency” (LipMetE) and a Matched Molecular Pairs Analysis

Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes

Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy

Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties

Total Synthesis of (+)-Phorboxazole A Exploiting the Petasis−Ferrier Rearrangement

Quantitative Assessment of the Impact of Fluorine Substitution on P‑Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

Strategies to optimize the brain availability of central nervous system drug candidates

Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand

Discovery of Clinical Candidate PF-06648671: A Potent γ‑Secretase Modulator for the Treatment of Alzheimer’s Disease

Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia

A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19

Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE

Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK

Design and Discovery of 6‑[(3S,4S)‑4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro‑2H‑pyran-4-yl)-1,5-dihydro‑4H‑pyrazolo[3,4‑d]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders

An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo

Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors

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