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Accurate and Reliable Prediction of Relative Ligand Binding Potency in Prospective Drug Discovery by Way of a Modern Free-Energy Calculation Protocol and Force Field

Journal of the American Chemical Society, 2015-02, Vol.137 (7), p.2695-2703

2015

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Selective interleukin-1 receptor-associated kinase 4 inhibitors for the treatment of autoimmune disorders and lymphoid malignancy

The Journal of experimental medicine, 2015-12, Vol.212 (13), p.2189-2201

2015

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Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279

Journal of medicinal chemistry, 2023-08, Vol.66 (15), p.10473-10496

2023

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Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.96-110

2015

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Human endogenous retrovirus-K (HERV-K) reverse transcriptase (RT) structure and biochemistry reveals remarkable similarities to HIV-1 RT and opportunities for HERV-K–specific inhibition

Proceedings of the National Academy of Sciences - PNAS, 2022-07, Vol.119 (27), p.1-e2200260119

2022

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Structures, functions and adaptations of the human LINE-1 ORF2 protein

Nature (London), 2024-02, Vol.626 (7997), p.194

2024

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Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders

Journal of medicinal chemistry, 2019-05, Vol.62 (10), p.4884-4901

2019

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Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis

Bioorganic & medicinal chemistry letters, 2022-10, Vol.73, p.128891-128891, Article 128891

2022

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A Stereoselective Intramolecular 1,3-Dipolar Nitrone Cycloaddition for the Synthesis of Substituted Chromanes

Journal of organic chemistry, 2002-05, Vol.67 (10), p.3317-3322

2002

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Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor

Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (16), p.4646-4649

2007

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Pd-Catalyzed Cycloisomerization to 1,2-Dialkylidenecycloalkanes. 2. Alternative Catalyst System

Journal of the American Chemical Society, 1994-05, Vol.116 (10), p.4268-4278

1994

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Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives

Journal of medicinal chemistry, 2000-03, Vol.43 (5), p.1034-1040

2000

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Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Journal of medicinal chemistry, 1994-04, Vol.37 (7), p.999-1014

1994

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Resistance mapping and mode of action of a novel class of antibacterial anthranilic acids: evidence for disruption of cell wall biosynthesis

Journal of antimicrobial chemotherapy, 2008-10, Vol.62 (4), p.720-729

2008

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Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation

Bioorganic & medicinal chemistry letters, 2006-12, Vol.16 (24), p.6173-6177

2006

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Preparation of novel anthranilic acids as antibacterial agents. Extensive evaluation of alternative amide bioisosteres connecting the A- and the B-rings

Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2823-2827

2007

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Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics

Bioorganic & medicinal chemistry letters, 2008-12, Vol.18 (23), p.6293-6297

2008

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Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles

Bioorganic & medicinal chemistry letters, 2007-04, Vol.17 (8), p.2347-2350

2007

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Structure–activity relationships of bioisosteres of a carboxylic acid in a novel class of bacterial translation inhibitors

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.4040-4043

2007

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Preparation of novel anthranilic acids as antibacterial agents: Extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity

Bioorganic & medicinal chemistry letters, 2007-06, Vol.17 (11), p.3113-3116

2007

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Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin‑1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders: Miniperspective

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.96-110

2015

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Correlation of carboxylic acid pKa to protein binding and antibacterial activity of a novel class of bacterial translation inhibitors

Bioorganic & medicinal chemistry letters, 2007-10, Vol.17 (19), p.5479-5482

2007

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Synthesis of N-substituted 1,2,5-thiadiazolidine and 1,2,6-thiadiazinane 1,1-dioxides from primary amines

Tetrahedron letters, 2003-07, Vol.44 (29), p.5483-5485

2003

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Kinetic studies with the non-nucleoside HIV-1 reverse transcriptase inhibitor U-88204E

Biochemistry (Easton), 1993-07, Vol.32 (26), p.6548-6554

1993

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The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity

Bioorganic & medicinal chemistry letters, 2000-04, Vol.10 (7), p.649-652

2000

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Accurate and Reliable Prediction of Relative Ligand Binding Potency in Prospective Drug Discovery by Way of a Modern Free-Energy Calculation Protocol and Force Field

Selective interleukin-1 receptor-associated kinase 4 inhibitors for the treatment of autoimmune disorders and lymphoid malignancy

Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279

Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders

Human endogenous retrovirus-K (HERV-K) reverse transcriptase (RT) structure and biochemistry reveals remarkable similarities to HIV-1 RT and opportunities for HERV-K–specific inhibition

Structures, functions and adaptations of the human LINE-1 ORF2 protein

Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders

Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis

A Stereoselective Intramolecular 1,3-Dipolar Nitrone Cycloaddition for the Synthesis of Substituted Chromanes

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor

Pd-Catalyzed Cycloisomerization to 1,2-Dialkylidenecycloalkanes. 2. Alternative Catalyst System

Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives

Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Resistance mapping and mode of action of a novel class of antibacterial anthranilic acids: evidence for disruption of cell wall biosynthesis

Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation

Preparation of novel anthranilic acids as antibacterial agents. Extensive evaluation of alternative amide bioisosteres connecting the A- and the B-rings

Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics

Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles

Structure–activity relationships of bioisosteres of a carboxylic acid in a novel class of bacterial translation inhibitors

Preparation of novel anthranilic acids as antibacterial agents: Extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity

Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin‑1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders: Miniperspective

Correlation of carboxylic acid pKa to protein binding and antibacterial activity of a novel class of bacterial translation inhibitors

Synthesis of N-substituted 1,2,5-thiadiazolidine and 1,2,6-thiadiazinane 1,1-dioxides from primary amines

Kinetic studies with the non-nucleoside HIV-1 reverse transcriptase inhibitor U-88204E

The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity

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