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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Chemical research in toxicology, 2004-01, Vol.17 (1), p.3-16

2004

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Escherichia coli Heat-Labile Enterotoxin B Limits T Cells Activation by Promoting Immature Dendritic Cells and Enhancing Regulatory T Cell Function

Frontiers in immunology, 2017-05, Vol.8, p.560-560

2017

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Reversal of High Fat Diet-Induced Obesity, Systemic Inflammation, and Astrogliosis by the NLRP3 Inflammasome Inhibitors NT-0249 and NT-0796

The Journal of pharmacology and experimental therapeutics, 2024-03, Vol.388 (3), p.813

2024

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The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1

Biochemical pharmacology, 2024-09, Vol.227, p.116455, Article 116455

2024

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Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders

Journal of medicinal chemistry, 2023-11, Vol.66 (21), p.14897-14911

2023

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Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency

The Journal of pharmacology and experimental therapeutics, 2024-03, Vol.388 (3), p.798

2024

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A quantitative high-throughput trapping assay as a measurement of potential for bioactivation

Analytical biochemistry, 2006-04, Vol.351 (2), p.266-272

2006

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Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors

Bioorganic & medicinal chemistry letters, 2020-12, Vol.30 (23), p.127560-127560, Article 127560

2020

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Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors

ACS medicinal chemistry letters, 2022-08, Vol.13 (8), p.1321-1328

2022

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Pharmacological Analysis of NLRP3 Inflammasome Inhibitor Sodium [(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl][(1-methyl‑1H‑pyrazol-4-yl)({[(2S)‑oxolan-2-yl]methyl})sulfamoyl]azanide in Cellular and Mouse Models of Inflammation Provides a Translational Framework

ACS pharmacology & translational science, 2024-05, Vol.7 (5), p.1438-1456

2024

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Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists

Journal of medicinal chemistry, 1997-12, Vol.40 (25), p.4053-4068

1997

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Approaches to higher-throughput pharmacokinetics (HTPK) in drug discovery

Drug Discovery Today, 2000, Vol.5 (1), p.17-24

2000

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Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets

Drug metabolism and disposition, 2003-06, Vol.31 (6), p.785

2003

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CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model

ACS medicinal chemistry letters, 2016-08, Vol.7 (8), p.768-773

2016

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Total Synthesis and Determination of the Absolute Configuration of Epibatidine

Journal of organic chemistry, 1994-04, Vol.59 (7), p.1771-1778

1994

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Controlled Modification of Acidity in Cholecystokinin B Receptor Antagonists: N-(1,4-Benzodiazepin-3-yl)-N ‘-[3-(tetrazol-5-ylamino)phenyl]ureas

Journal of medicinal chemistry, 1996-02, Vol.39 (4), p.842-849

1996

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Chiral Base-Mediated Asymmetric Synthesis of Tricarbonyl(.eta.6-arene)chromium Complexes

Journal of organic chemistry, 1994-04, Vol.59 (8), p.1961-1962

1994

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Higher Throughput Bioanalysis by Automation of a Protein Precipitation Assay Using a 96-Well Format with Detection by LC−MS/MS

Analytical chemistry (Washington), 2000-03, Vol.72 (5), p.979-984

2000

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Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles

Journal of medicinal chemistry, 1999-06, Vol.42 (12), p.2087-2104

1999

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A Randomized, Double-Blind, Crossover Comparison of MK-0929 and Placebo in the Treatment of Adults With ADHD

Journal of attention disorders, 2012-11, Vol.16 (8), p.664-674

2012

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Identification of metabolites of a substance P (neurokinin 1 receptor) antagonist in rat hepatocytes and rat plasma

Drug metabolism and disposition, 2002-08, Vol.30 (8), p.937

2002

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Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor

The Journal of pharmacology and experimental therapeutics, 1997-11, Vol.283 (2), p.636

1997

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An Evaluation of a Four-Channel Multiplexed Electrospray Tandem Mass Spectrometry for Higher Throughput Quantitative Analysis

Analytical chemistry (Washington), 2002-04, Vol.74 (8), p.1896-1902

2002

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2-Aryl indole NK1 receptor antagonists : Optimisation of indole substitution

Bioorganic & medicinal chemistry letters, 2001-05, Vol.11 (9), p.1233-1236

2001

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Determination of drug concentrations in plasma by a highly automated, generic and flexible protein precipitation and liquid chromatography/tandem mass spectrometry method applicable to the drug discovery environment

Rapid communications in mass spectrometry, 2002-01, Vol.16 (11), p.1065-1071

2002

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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Escherichia coli Heat-Labile Enterotoxin B Limits T Cells Activation by Promoting Immature Dendritic Cells and Enhancing Regulatory T Cell Function

Reversal of High Fat Diet-Induced Obesity, Systemic Inflammation, and Astrogliosis by the NLRP3 Inflammasome Inhibitors NT-0249 and NT-0796

The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1

Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders

Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency

A quantitative high-throughput trapping assay as a measurement of potential for bioactivation

Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors

Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors

Pharmacological Analysis of NLRP3 Inflammasome Inhibitor Sodium [(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl][(1-methyl‑1H‑pyrazol-4-yl)({[(2S)‑oxolan-2-yl]methyl})sulfamoyl]azanide in Cellular and Mouse Models of Inflammation Provides a Translational Framework

Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists

Approaches to higher-throughput pharmacokinetics (HTPK) in drug discovery

Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets

CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model

Total Synthesis and Determination of the Absolute Configuration of Epibatidine

Controlled Modification of Acidity in Cholecystokinin B Receptor Antagonists: N-(1,4-Benzodiazepin-3-yl)-N ‘-[3-(tetrazol-5-ylamino)phenyl]ureas

Chiral Base-Mediated Asymmetric Synthesis of Tricarbonyl(.eta.6-arene)chromium Complexes

Higher Throughput Bioanalysis by Automation of a Protein Precipitation Assay Using a 96-Well Format with Detection by LC−MS/MS

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles

A Randomized, Double-Blind, Crossover Comparison of MK-0929 and Placebo in the Treatment of Adults With ADHD

Identification of metabolites of a substance P (neurokinin 1 receptor) antagonist in rat hepatocytes and rat plasma

Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor

An Evaluation of a Four-Channel Multiplexed Electrospray Tandem Mass Spectrometry for Higher Throughput Quantitative Analysis

2-Aryl indole NK1 receptor antagonists : Optimisation of indole substitution

Determination of drug concentrations in plasma by a highly automated, generic and flexible protein precipitation and liquid chromatography/tandem mass spectrometry method applicable to the drug discovery environment

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