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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8806-8817

2015

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Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors

Journal of medicinal chemistry, 2017-02, Vol.60 (4), p.1262-1271

2017

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Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Journal of medicinal chemistry, 2020-07, Vol.63 (14), p.7510-7528

2020

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Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13578-13594

2020

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Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective

Journal of medicinal chemistry, 2020-12, Vol.63 (23), p.14197-14215

2020

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Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment

Journal of medicinal chemistry, 2015-02, Vol.58 (3), p.1038-1052

2015

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Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)

Journal of medicinal chemistry, 2020-12, Vol.63 (23), p.14522-14529

2020

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Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11368-11396

2020

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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Journal of medicinal chemistry, 2017-11, Vol.60 (22), p.9184-9204

2017

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Overview of the Development of Glutaminase Inhibitors: Achievements and Future Directions

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1096-1115

2019

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Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity

Journal of medicinal chemistry, 2018-06, Vol.61 (11), p.4883-4903

2018

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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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Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Journal of medicinal chemistry, 2015-12, Vol.58 (24), p.9421-9437

2015

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Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)‑3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)‑ol (GSK656)

Journal of medicinal chemistry, 2017-10, Vol.60 (19), p.8011-8026

2017

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Design and Synthesis of Potent and Multifunctional Aldose Reductase Inhibitors Based on Quinoxalinones

Journal of medicinal chemistry, 2015-02, Vol.58 (3), p.1254-1267

2015

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Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)‑1-((S)‑2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy‑N‑(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.599-618

2018

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Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders

Journal of medicinal chemistry, 2020-09, Vol.63 (17), p.9977-9989

2020

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Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.184-215

2021

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Macrocycles Are Great Cycles: Applications, Opportunities, and Challenges of Synthetic Macrocycles in Drug Discovery

Journal of medicinal chemistry, 2011-04, Vol.54 (7), p.1961-2004

2011

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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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PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2091-2113

2015

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High-Throughput Screening for the Discovery of Enzyme Inhibitors

Journal of medicinal chemistry, 2020-10, Vol.63 (19), p.10742-10772

Lloyd, Matthew D

2020

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Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

Journal of medicinal chemistry, 2020-10, Vol.63 (19), p.10984-11011

2020

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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist

Journal of medicinal chemistry, 2024-05, Vol.67 (9), p.7245-7259

2024

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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer

Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment

Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)

Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Overview of the Development of Glutaminase Inhibitors: Achievements and Future Directions

Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3‑(5-Fluoro‑1H‑indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)‑3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)‑ol (GSK656)

Design and Synthesis of Potent and Multifunctional Aldose Reductase Inhibitors Based on Quinoxalinones

Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders

Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products

Macrocycles Are Great Cycles: Applications, Opportunities, and Challenges of Synthetic Macrocycles in Drug Discovery

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

PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS

High-Throughput Screening for the Discovery of Enzyme Inhibitors

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist

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