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Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRβ

Bioorganic & medicinal chemistry, 2009-05, Vol.17 (10), p.3519-3527

2009

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Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood–brain penetration

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.689-693

2010

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Carboxylic acid based quinolines as liver X receptor modulators that have LXRβ receptor binding selectivity

Bioorganic & medicinal chemistry, 2008, Vol.18 (1), p.54-59

2008

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Discovery of Phenyl Acetic Acid Substituted Quinolines as Novel Liver X Receptor Agonists for the Treatment of Atherosclerosis

Journal of medicinal chemistry, 2006-10, Vol.49 (21), p.6151-6154

2006

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Discovery and initial optimization of 5,5′-disubstituted aminohydantoins as potent β-secretase (BACE1) inhibitors

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.632-635

2010

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Further modification on phenyl acetic acid based quinolines as liver X receptor modulators

Bioorganic & medicinal chemistry, 2007-05, Vol.15 (10), p.3321-3333

2007

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Synthesis and Structure−Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis

Journal of medicinal chemistry, 2003-06, Vol.46 (12), p.2361-2375

2003

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Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (13), p.3457-3460

2004

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Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy

Journal of medicinal chemistry, 2021-04, Vol.64 (7), p.3843-3869

2021

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Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase

Journal of medicinal chemistry, 2018-08, Vol.61 (15), p.6801-6813

2018

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Novel (4-piperidin-1-yl)-phenyl sulfonamides as potent and selective human β3 agonists

Bioorganic & medicinal chemistry, 2001-08, Vol.9 (8), p.2045-2059

2001

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2,4-Thiazolidinediones as potent and selective human β3 agonists

Bioorganic & medicinal chemistry letters, 2001-03, Vol.11 (6), p.757-760

2001

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Orally Bioavailable β3-Adrenergic Receptor Agonists as Potential Therapeutic Agents for Obesityand Type-II Diabetes

Progress in Medicinal Chemistry, 2003, Vol.41, p.167-194

2003

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New oxadiazolidinedione derivatives as potent and selective human β3 agonists

Bioorganic & medicinal chemistry letters, 2001-04, Vol.11 (8), p.981-984

2001

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Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1

Bioorganic & medicinal chemistry letters, 2005-08, Vol.15 (15), p.3514-3518

2005

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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1

ACS medicinal chemistry letters, 2024-09, Vol.15 (9), p.1606-1614

2024

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Structure-Based Approach To Identify 5‑[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.6451-6457

2017

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Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)

ACS medicinal chemistry letters, 2022-01, Vol.13 (1), p.84-91

2022

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Tetrahydroindazoles as Interleukin‑2 Inducible T‑Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo

Journal of medicinal chemistry, 2015-05, Vol.58 (9), p.3806-3816

2015

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(4-Piperidin-1-yl)phenyl Amides: Potent and Selective Human β3 Agonists

Journal of medicinal chemistry, 2001-04, Vol.44 (9), p.1456-1466

2001

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Synthesis of Heterocycle Substituted 1-Aryl-4-piperidones

Heterocycles, 2002-05, Vol.57 (5), p.857

2002

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Carbenoid versus Vinylogous Reactivity in Rhodium(II)-Stabilized Vinylcarbenoids

Journal of organic chemistry, 1994-08, Vol.59 (16), p.4535-4541

1994

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Identification of Phenylsulfone-Substituted Quinoxaline (WYE-672) as a Tissue Selective Liver X-receptor (LXR) Agonist

Journal of medicinal chemistry, 2010-04, Vol.53 (8), p.3296-3304

2010

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Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRβ

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood–brain penetration

Carboxylic acid based quinolines as liver X receptor modulators that have LXRβ receptor binding selectivity

Discovery of Phenyl Acetic Acid Substituted Quinolines as Novel Liver X Receptor Agonists for the Treatment of Atherosclerosis

Discovery and initial optimization of 5,5′-disubstituted aminohydantoins as potent β-secretase (BACE1) inhibitors

Further modification on phenyl acetic acid based quinolines as liver X receptor modulators

Synthesis and Structure−Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis

Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase

Novel (4-piperidin-1-yl)-phenyl sulfonamides as potent and selective human β3 agonists

2,4-Thiazolidinediones as potent and selective human β3 agonists

Orally Bioavailable β3-Adrenergic Receptor Agonists as Potential Therapeutic Agents for Obesityand Type-II Diabetes

New oxadiazolidinedione derivatives as potent and selective human β3 agonists

Discovery of a Potent (4R,5S)‑4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling

Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1

Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1

Structure-Based Approach To Identify 5‑[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators

Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)

Tetrahydroindazoles as Interleukin‑2 Inducible T‑Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo

(4-Piperidin-1-yl)phenyl Amides: Potent and Selective Human β3 Agonists

Synthesis of Heterocycle Substituted 1-Aryl-4-piperidones

Carbenoid versus Vinylogous Reactivity in Rhodium(II)-Stabilized Vinylcarbenoids

Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic Acid, Efipladib

Identification of Phenylsulfone-Substituted Quinoxaline (WYE-672) as a Tissue Selective Liver X-receptor (LXR) Agonist

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