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A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation

Cell chemical biology, 2016-11, Vol.23 (11), p.1362-1371

2016

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Trends in covalent drug discovery: a 2020-23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs

Expert opinion on therapeutic patents, 2024-10, Vol.34 (10), p.843

2024

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A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

Nature chemical biology, 2014-08, Vol.10 (8), p.629-631

2014

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Diabetes area patent participation analysis - part II: years 2011-2016

Expert opinion on therapeutic patents, 2018-02, Vol.28 (2), p.111-122

2018

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Diabetes area participation analysis: a review of companies and targets described in the 2008 - 2010 patent literature

Expert opinion on therapeutic patents, 2010-12, Vol.20 (12), p.1627-1651

2010

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Latest approaches for the treatment of obesity

Expert opinion on drug discovery, 2015-08, Vol.10 (8), p.825-839

2015

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Mechanistic Characterization of a 2‑Thioxanthine Myeloperoxidase Inhibitor and Selectivity Assessment Utilizing Click Chemistry–Activity-Based Protein Profiling

Biochemistry (Easton), 2013-12, Vol.52 (51), p.9187-9201

2013

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Investigational drugs in Phase II clinical trials for the treatment of obesity: implications for future development of novel therapies

Expert opinion on investigational drugs, 2014-08, Vol.23 (8), p.1055-1066

2014

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Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution

Bioorganic & medicinal chemistry, 2017-02, Vol.25 (3), p.1000-1003

2017

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Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries

Bioorganic & medicinal chemistry letters, 2013-03, Vol.23 (5), p.1407-1411

2013

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Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylamino-piperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

Journal of medicinal chemistry, 2009-01, Vol.52 (2), p.234-237

2009

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Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

Journal of medicinal chemistry, 2009-01, Vol.52 (2), p.234-237

2009

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Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7164-7172

2015

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MAP4K4 Is a Threonine Kinase That Phosphorylates FARP1

ACS chemical biology, 2015-12, Vol.10 (12), p.2667-2671

2015

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Development of a selective activity-based probe for glycosylated LIPA

Bioorganic & medicinal chemistry letters, 2016-04, Vol.26 (8), p.1993-1996

2016

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Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7173-7185

2015

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Deconstruction of Activity-Dependent Covalent Modification of Heme in Human Neutrophil Myeloperoxidase by Multistage Mass Spectrometry (MS4)

Biochemistry (Easton), 2012-03, Vol.51 (10), p.2065-2077

2012

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Discovery of 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based Cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

Journal of medicinal chemistry, 2009-05, Vol.52 (9), p.2652-2655

2009

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Discovery and in Vitro Optimization of 3‑Sulfamoylbenzamides as ROMK Inhibitors

ACS medicinal chemistry letters, 2018-02, Vol.9 (2), p.125-130

2018

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Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (8), p.2738-2743

2012

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Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (13), p.4281-4287

2012

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Discovery and evaluation of pyrazolo[1,5- a]pyrimidines as neuropeptide Y1 receptor antagonists

Bioorganic & medicinal chemistry letters, 2011-05, Vol.21 (9), p.2641-2645

2011

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Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents

ACS medicinal chemistry letters, 2012-05, Vol.3 (5), p.397-401

2012

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A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation

Trends in covalent drug discovery: a 2020-23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs

A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms

Diabetes area patent participation analysis - part II: years 2011-2016

Diabetes area participation analysis: a review of companies and targets described in the 2008 - 2010 patent literature

Latest approaches for the treatment of obesity

Mechanistic Characterization of a 2‑Thioxanthine Myeloperoxidase Inhibitor and Selectivity Assessment Utilizing Click Chemistry–Activity-Based Protein Profiling

Investigational drugs in Phase II clinical trials for the treatment of obesity: implications for future development of novel therapies

Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution

Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries

Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylamino-piperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3

MAP4K4 Is a Threonine Kinase That Phosphorylates FARP1

Development of a selective activity-based probe for glycosylated LIPA

Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)

Discovery of 2‑(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)‑yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases

Deconstruction of Activity-Dependent Covalent Modification of Heme in Human Neutrophil Myeloperoxidase by Multistage Mass Spectrometry (MS4)

Discovery of 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based Cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

Discovery and in Vitro Optimization of 3‑Sulfamoylbenzamides as ROMK Inhibitors

Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor

Discovery and evaluation of pyrazolo[1,5- a]pyrimidines as neuropeptide Y1 receptor antagonists

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents

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