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Identification of (R)‑N‑((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)‑1H‑indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B‑Cell Lymphomas

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9928-9941

2016

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Histone Modifications and Cancer

Cold Spring Harbor perspectives in biology, 2016-04, Vol.8 (4), p.a019521-a019521

2016

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Collaboration and knowledge integration for successful brain therapeutics - lessons learned from the pandemic

Disease models & mechanisms, 2022-12, Vol.15 (12)

2022

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Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

ACS medicinal chemistry letters, 2014-04, Vol.5 (4), p.378-383

2014

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Preparation and biological evaluation of conformationally constrained BACE1 inhibitors

Bioorganic & medicinal chemistry, 2015-07, Vol.23 (13), p.3260-3268

2015

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Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

ACS medicinal chemistry letters, 2016-02, Vol.7 (2), p.145-150

2016

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Ilaprazole and Other Novel Prazole-Based Compounds That Bind Tsg101 Inhibit Viral Budding of Herpes Simplex Virus 1 and 2 and Human Immunodeficiency Virus from Cells

Journal of virology, 2021-05, Vol.95 (11)

2021

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Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

The Journal of neuroscience, 2011-11, Vol.31 (46), p.16507-16516

2011

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Mentoring Matters in Drug Discovery

ACS medicinal chemistry letters, 2020-03, Vol.11 (3), p.241-244

2020

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Comparison of the effects of serotonin selective, norepinephrine selective, and dual serotonin and norepinephrine reuptake inhibitors on lower urinary tract function in cats

Life sciences (1973), 2002-08, Vol.71 (11), p.1227-1236

2002

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Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity

The Journal of biological chemistry, 2021-01, Vol.296, p.100349, Article 100349

2021

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Identification of potent, selective KDM5 inhibitors

Bioorganic & medicinal chemistry letters, 2016-09, Vol.26 (17), p.4350-4354

2016

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Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints

Bioorganic & medicinal chemistry, 2020-01, Vol.28 (1), p.115194, Article 115194

2020

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Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

ACS medicinal chemistry letters, 2020-06, Vol.11 (6), p.1205-1212

2020

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Early Drug‐Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors

ChemMedChem, 2020-06, Vol.15 (11), p.955-960

2020

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Discovery, design, and synthesis of indole-based EZH2 inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3644-3649

2015

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[3H]LY334370, a novel radioligand for the 5-HT1F receptor. II. Autoradiographic localization in rat, guinea pig, monkey and human brain

Naunyn-Schmiedeberg's archives of pharmacology, 2005-03, Vol.371 (3), p.178-184

2005

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A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation

Organic letters, 2014-08, Vol.16 (16), p.4114-4117

2014

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In vivo assessment of brain interstitial fluid with microdialysis reveals plaque-associated changes in amyloid-beta metabolism and half-life

The Journal of neuroscience, 2003-10, Vol.23 (26), p.8844-8853

2003

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Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

ACS medicinal chemistry letters, 2020-06, Vol.11 (6), p.1213-1220

2020

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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

Histone Modifications and Cancer

Collaboration and knowledge integration for successful brain therapeutics - lessons learned from the pandemic

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

Preparation and biological evaluation of conformationally constrained BACE1 inhibitors

Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

Ilaprazole and Other Novel Prazole-Based Compounds That Bind Tsg101 Inhibit Viral Budding of Herpes Simplex Virus 1 and 2 and Human Immunodeficiency Virus from Cells

The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

Mentoring Matters in Drug Discovery

Comparison of the effects of serotonin selective, norepinephrine selective, and dual serotonin and norepinephrine reuptake inhibitors on lower urinary tract function in cats

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition

Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity

Identification of potent, selective KDM5 inhibitors

Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints

Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

Early Drug‐Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors

Discovery, design, and synthesis of indole-based EZH2 inhibitors

[3H]LY334370, a novel radioligand for the 5-HT1F receptor. II. Autoradiographic localization in rat, guinea pig, monkey and human brain

A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1‑like

In vivo assessment of brain interstitial fluid with microdialysis reveals plaque-associated changes in amyloid-beta metabolism and half-life

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

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