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Structural and Functional Basis of Cyclooxygenase Inhibition

Journal of medicinal chemistry, 2007-04, Vol.50 (7), p.1425-1441

2007

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Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain

Proceedings of the National Academy of Sciences - PNAS, 2017-03, Vol.114 (10), p.E1996-E2005

2017

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Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992

Molecular pharmacology, 2018-08, Vol.94 (2), p.926-937

2018

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Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.9027-9040

2015

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Selective Visualization of Cyclooxygenase-2 in Inflammation and Cancer by Targeted Fluorescent Imaging Agents

Cancer research (Chicago, Ill.), 2010-05, Vol.70 (9), p.3618-3627

2010

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Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant)

Drug metabolism and disposition, 2017-12, Vol.45 (12), p.1245-1259

2017

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ortho-Carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors

Bioorganic & medicinal chemistry, 2012-08, Vol.20 (15), p.4830-4837

2012

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Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6‑((1H‑Pyrazolo[4,3‑b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4)

Journal of medicinal chemistry, 2019-01, Vol.62 (1), p.342-358

2019

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Cyclooxygenase-1-Selective Inhibitors Based on the (E)-2′-Des-methyl-sulindac Sulfide Scaffold

Journal of medicinal chemistry, 2012-03, Vol.55 (5), p.2287-2300

2012

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Design and Synthesis of N‑Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.925-930

2017

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Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

ACS medicinal chemistry letters, 2017-02, Vol.8 (2), p.233-238

2017

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Molecular Determinants for the Selective Inhibition of Cyclooxygenase-2 by Lumiracoxib

The Journal of biological chemistry, 2007-06, Vol.282 (22), p.16379-16390

2007

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Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.5084-5088

2012

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The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5

Drug metabolism and disposition, 2012-09, Vol.40 (9), p.1834

2012

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Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

Molecular psychiatry, 2020-11, Vol.25 (11), p.2786-2799

2020

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Sterol 14α-Demethylase Structure-Based Design of VNI ((R)‑N‑(1-(2,4-Dichlorophenyl)-2-(1H‑imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis

Journal of medicinal chemistry, 2018-07, Vol.61 (13), p.5679-5691

2018

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Targeting Selective Activation of M1 for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M1 Positive Allosteric Modulator ML169

ACS chemical neuroscience, 2012-07, Vol.3 (11), p.884-895

2012

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Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy

ACS medicinal chemistry letters, 2020-01, Vol.11 (1), p.29-33

2020

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Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro

Bioorganic & medicinal chemistry letters, 2022-10, Vol.74, p.128923-128923, Article 128923

2022

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Modulation of arousal and sleep/wake architecture by M1 PAM VU0453595 across young and aged rodents and nonhuman primates

Neuropsychopharmacology (New York, N.Y.), 2020-12, Vol.45 (13), p.2219-2228

2020

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Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists

Bioorganic & medicinal chemistry letters, 2022-12, Vol.78, p.129021-129021, Article 129021

2022

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Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7485-7500

2015

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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu 7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1690-1695

2019

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Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128193-128193, Article 128193

2021

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Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (22), p.127529-127529, Article 127529

2020

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Structural and Functional Basis of Cyclooxygenase Inhibition

Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain

Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992

Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Selective Visualization of Cyclooxygenase-2 in Inflammation and Cancer by Targeted Fluorescent Imaging Agents

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant)

ortho-Carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors

Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6‑((1H‑Pyrazolo[4,3‑b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4)

Cyclooxygenase-1-Selective Inhibitors Based on the (E)-2′-Des-methyl-sulindac Sulfide Scaffold

Design and Synthesis of N‑Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

Molecular Determinants for the Selective Inhibition of Cyclooxygenase-2 by Lumiracoxib

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

Sterol 14α-Demethylase Structure-Based Design of VNI ((R)‑N‑(1-(2,4-Dichlorophenyl)-2-(1H‑imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis

Targeting Selective Activation of M1 for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M1 Positive Allosteric Modulator ML169

Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy

Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro

Modulation of arousal and sleep/wake architecture by M1 PAM VU0453595 across young and aged rodents and nonhuman primates

Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu 7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)

Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1

Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core

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