Publications by authors named "Patrick Verhoest"

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Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease.
Jamison B Tuttle, Christophe Allais, Charlotte M N Allerton, Annaliesa S Anderson, Joel T Arcari, Patrick R Verhoest

J Med Chem· April 2025

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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Charlotte M N Allerton, Joel T Arcari, Lisa M Aschenbrenner, Melissa Avery, Bruce M Bechle, Patrick R Verhoest

J Med Chem· August 2024

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Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Martin Pettersson, Douglas S Johnson, John M Humphrey, Christopher W Am Ende, Todd W Butler, Patrick R Verhoest

J Med Chem· June 2024

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Designing small molecules for therapeutic success: A contemporary perspective.
Tristan S Maurer, Martin Edwards, David Hepworth, Patrick Verhoest, Charlotte M N Allerton

Drug Discov Today· February 2022

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Innovation in breakthrough drugs and vaccines: Development risk, patient impact, and value.
Andrew E Prigodich, Shuntai Wang, Patrick Verhoest, Nicholas Warne, Charlotte Allerton

Drug Discov Today· October 2021

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Harnessing Preclinical Data as a Predictive Tool for Human Brain Tissue Targeting.
Nandini C Patel, Bo Feng, Xinjun Hou, Mark A West, Patrick E Trapa, Patrick Verhoest

ACS Chem Neurosci· March 2021

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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Uthpala Seneviratne, Zhen Huang, Christopher W Am Ende, Todd W Butler, Leah Cleary, Patrick R Verhoest

Cell Chem Biol· February 2021

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Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition.
Cheng Chang, Kari R Fonseca, Cheryl Li, Weldon Horner, Laura E Zawadzke, Patrick Verhoest

Mol Pharmacol· August 2018

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Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Christopher J Helal, Eric P Arnold, Tracey L Boyden, Cheng Chang, Thomas A Chappie, Patrick R Verhoest

J Med Chem· April 2018

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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Christopher J Helal, Eric Arnold, Tracey Boyden, Cheng Chang, Thomas A Chappie, Patrick R Verhoest

J Med Chem· February 2018

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Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Antonia F Stepan, Tuan P Tran, Christopher J Helal, Maria S Brown, Cheng Chang, Patrick R Verhoest

ACS Med Chem Lett· February 2018

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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.
Lei Zhang, Laigao Chen, Elizabeth M Beck, Thomas A Chappie, Richard V Coelho, Patrick R Verhoest

J Med Chem· October 2017

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Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Antonia F Stepan, Michelle M Claffey, Matthew R Reese, Gayatri Balan, Gabriela Barreiro, Patrick R Verhoest

J Med Chem· September 2017

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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Christopher J Helal, Eric P Arnold, Tracey L Boyden, Cheng Chang, Thomas A Chappie, Patrick R Verhoest

J Med Chem· July 2017

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Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.
Martin Pettersson, Douglas S Johnson, Danica A Rankic, Gregory W Kauffman, Christopher W Am Ende, Patrick R Verhoest

Medchemcomm· April 2017

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Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery.
Travis T Wager, Xinjun Hou, Patrick R Verhoest, Anabella Villalobos

ACS Chem Neurosci· June 2016

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Quantitative Assessment of the Impact of Fluorine Substitution on P-Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability.
Martin Pettersson, Xinjun Hou, Max Kuhn, Travis T Wager, Gregory W Kauffman, Patrick R Verhoest

J Med Chem· June 2016

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Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK.
Qi Wang, Stephen P Amato, David M Rubitski, Matthew M Hayward, Bethany L Kormos, Patrick R Verhoest

J Pharmacol Exp Ther· February 2016

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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway.
Amy B Dounay, Jamison B Tuttle, Patrick R Verhoest

J Med Chem· November 2015

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Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.
Martin Pettersson, Douglas S Johnson, John M Humphrey, Todd W Butler, Christopher W Am Ende, Patrick R Verhoest

ACS Med Chem Lett· May 2015

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Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.
Martin Pettersson, Douglas S Johnson, John M Humphrey, Christopher W Am Ende, Edelweiss Evrard, Patrick R Verhoest

Bioorg Med Chem Lett· February 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.
Jaclyn L Henderson, Bethany L Kormos, Matthew M Hayward, Karen J Coffman, Jayasankar Jasti, Patrick R Verhoest

J Med Chem· January 2015

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Chemoproteomics demonstrates target engagement and exquisite selectivity of the clinical phosphodiesterase 10A inhibitor MP-10 in its native environment.
Jan-Philip Schülke, Laura A McAllister, Kieran F Geoghegan, Vinod Parikh, Thomas A Chappie, Patrick R Verhoest

ACS Chem Biol· December 2014

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Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.
Paul Galatsis, Jaclyn L Henderson, Bethany L Kormos, Seungil Han, Ravi G Kurumbail, Patrick R Verhoest

Bioorg Med Chem Lett· September 2014

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