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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Science translational medicine, 2016-11, Vol.8 (363), p.363ra150

2016

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Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression

Nature communications, 2019-05, Vol.10 (1), p.2261-2261, Article 2261

2019

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Structure-function analysis of the SHOC2-MRAS-PP1C holophosphatase complex

Nature (London), 2022-09, Vol.609 (7926), p.408-415

2022

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Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

Bioorganic & medicinal chemistry letters, 2019-09, Vol.29 (17), p.2503-2510

2019

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Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.2983-2992

2017

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Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

Cancer research (Chicago, Ill.), 2021-04, Vol.81 (8), p.2002-2014

2021

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A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors

ACS medicinal chemistry letters, 2022-03, Vol.13 (3), p.377-387

2022

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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (7), p.2444-2449

2012

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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055

ACS medicinal chemistry letters, 2024-04, Vol.15 (4), p.524-532

2024

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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors

ACS medicinal chemistry letters, 2017-12, Vol.8 (12), p.1292-1297

2017

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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10700-10708

2018

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Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

Experimental neurology, 2010-10, Vol.225 (2), p.384-390

2010

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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (5), p.1376-1380

2007

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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

Experimental neurology, 2010-10, Vol.225 (2), p.384

2010

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CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

The Journal of neuroscience, 2014-06, Vol.34 (24), p.8336-8346

2014

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Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Journal of medicinal chemistry, 2010-02, Vol.53 (3), p.942-950

2010

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A Novel Method for the Preparation of 4‑Arylimidazolones

Organic letters, 2013-06, Vol.15 (11), p.2830-2833

2013

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Formal Olefination and Acylaziridination of Imidazolones

Organic letters, 2010-06, Vol.12 (12), p.2718-2721

2010

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Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story

Current opinion in chemical biology, 2013-06, Vol.17 (3), p.320-328

2013

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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

ACS medicinal chemistry letters, 2012-11, Vol.3 (11), p.897-902

2012

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Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

ACS medicinal chemistry letters, 2018-05, Vol.9 (5), p.457-461

2018

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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression

Structure-function analysis of the SHOC2-MRAS-PP1C holophosphatase complex

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia

Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055

Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

A Novel Method for the Preparation of 4‑Arylimidazolones

Formal Olefination and Acylaziridination of Imidazolones

Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

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