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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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Molecular Shape and Medicinal Chemistry: A Perspective

Journal of medicinal chemistry, 2010-05, Vol.53 (10), p.3862-3886

2010

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Bicyclic Helical Peptides as Dual Inhibitors Selective for Bcl2A1 and Mcl‑1 Proteins

Journal of medicinal chemistry, 2018-04, Vol.61 (7), p.2962-2972

2018

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Optimization of CAMD techniques 3. Virtual screening enrichment studies: a help or hindrance in tool selection?

Journal of computer-aided molecular design, 2008-03, Vol.22 (3-4), p.169-178

2008

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

Journal of medicinal chemistry, 2016-06, Vol.59 (11), p.5391-5402

2016

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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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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1

Journal of medicinal chemistry, 2022-08, Vol.65 (16), p.11177-11186

2022

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Discovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1708-1729

2014

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Electrophilic Helical Peptides That Bond Covalently, Irreversibly, and Selectively in a Protein–Protein Interaction Site

ACS medicinal chemistry letters, 2017-01, Vol.8 (1), p.22-26

2017

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Implications of Promiscuous Pim-1 Kinase Fragment Inhibitor Hydrophobic Interactions for Fragment-Based Drug Design

Journal of medicinal chemistry, 2012-03, Vol.55 (6), p.2641-2648

2012

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Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor

ACS medicinal chemistry letters, 2018-02, Vol.9 (2), p.143-148

2018

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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9208-9223

2012

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P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1853-1859

2018

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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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Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus

Bioorganic & medicinal chemistry letters, 2017-02, Vol.27 (3), p.590-596

2017

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Hepatitis C Virus NS5A Replication Complex Inhibitors. Part 6: Discovery of a Novel and Highly Potent Biarylimidazole Chemotype with Inhibitory Activity Toward Genotypes 1a and 1b Replicons

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1995-2012

2014

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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE)

Bioorganic & medicinal chemistry letters, 2015-11, Vol.25 (22), p.5040-5047

2015

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An Empirical Process for the Design of High-Throughput Screening Deck Filters

Journal of chemical information and modeling, 2006-05, Vol.46 (3), p.1060-1068

2006

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HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.779-784

2013

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Measuring CAMD technique performance: A virtual screening case study in the design of validation experiments

Journal of computer-aided molecular design, 2004-07, Vol.18 (7-9), p.529-536

2004

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Incidence and characterization of diagnosed endometriosis in a geographically defined population

Fertility and sterility, 2004-08, Vol.82 (2), p.314-321

2004

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HCV NS5A replication complex inhibitors. Part 5: Discovery of potent and pan-genotypic glycinamide cap derivatives

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (15), p.4428-4435

2013

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Measuring CAMD Technique Performance. 2. How “Druglike” Are Drugs? Implications of Random Test Set Selection Exemplified Using Druglikeness Classification Models

Journal of chemical information and modeling, 2007-01, Vol.47 (1), p.110-114

2007

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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (22), p.6916-6924

2011

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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (22), p.6909-6915

2011

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Molecular Shape and Medicinal Chemistry: A Perspective

Bicyclic Helical Peptides as Dual Inhibitors Selective for Bcl2A1 and Mcl‑1 Proteins

Optimization of CAMD techniques 3. Virtual screening enrichment studies: a help or hindrance in tool selection?

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

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

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1

Discovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection

Electrophilic Helical Peptides That Bond Covalently, Irreversibly, and Selectively in a Protein–Protein Interaction Site

Implications of Promiscuous Pim-1 Kinase Fragment Inhibitor Hydrophobic Interactions for Fragment-Based Drug Design

Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor

Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus

Hepatitis C Virus NS5A Replication Complex Inhibitors. Part 6: Discovery of a Novel and Highly Potent Biarylimidazole Chemotype with Inhibitory Activity Toward Genotypes 1a and 1b Replicons

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE)

An Empirical Process for the Design of High-Throughput Screening Deck Filters

HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies

Measuring CAMD technique performance: A virtual screening case study in the design of validation experiments

Incidence and characterization of diagnosed endometriosis in a geographically defined population

HCV NS5A replication complex inhibitors. Part 5: Discovery of potent and pan-genotypic glycinamide cap derivatives

Measuring CAMD Technique Performance. 2. How “Druglike” Are Drugs? Implications of Random Test Set Selection Exemplified Using Druglikeness Classification Models

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors

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