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Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex

Communications chemistry, 2024-08, Vol.7 (1), p.183-16

2024

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Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels

The Journal of neuroscience, 2008-05, Vol.28 (19), p.5063-5071

2008

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Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy

Journal of the American Chemical Society, 2003-04, Vol.125 (14), p.4087-4096

2003

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Fragment Screening and Assembly: A Highly Efficient Approach to a Selective and Cell Active Protein Tyrosine Phosphatase 1B Inhibitor

Journal of medicinal chemistry, 2003-09, Vol.46 (20), p.4232-4235

2003

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Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Behavior

Journal of the American Chemical Society, 2021-10, Vol.143 (42), p.17479-17491

2021

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CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16

ACS chemical biology, 2023-02, Vol.18 (2), p.331-339

2023

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Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer’s Disease: 2‑(3-Phenyl‑1H‑pyrazol-1-yl)-nicotinamides

Journal of medicinal chemistry, 2017-08, Vol.60 (16), p.7123-7138

2017

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Current status and future prospects for enabling chemistry technology in the drug discovery process [version 1; peer review: 2 approved]

F1000 research, 2016, Vol.5, p.2426-2426

2016

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Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo

Journal of medicinal chemistry, 2023-03, Vol.66 (6), p.3852-3865

2023

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Ligand association rates to the inner-variable-domain of a dual-variable-domain immunoglobulin are significantly impacted by linker design

mAbs, 2011-09, Vol.3 (5), p.487-494

2011

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Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists

Bioorganic & medicinal chemistry letters, 2018-10, Vol.28 (19), p.3260-3264

2018

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Analgesic potential of TRPV1 antagonists

Biochemical pharmacology, 2009-08, Vol.78 (3), p.211-216

2009

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Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds

Journal of medicinal chemistry, 2024-04, Vol.67 (8), p.6456-6494

2024

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1804-1810

2018

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Identification of a monoacid-Based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B

Bioorganic & medicinal chemistry letters, 2003-11, Vol.13 (22), p.3947-3950

2003

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Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity

Journal of medicinal chemistry, 2006-06, Vol.49 (12), p.3563-3580

2006

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Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8

ACS medicinal chemistry letters, 2016-12, Vol.7 (12), p.1102-1106

2016

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Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1682-1685

2009

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Selective Protein Tyrosine Phosphatase 1B Inhibitors: Targeting the Second Phosphotyrosine Binding Site with Non-Carboxylic Acid-Containing Ligands

Journal of medicinal chemistry, 2003-07, Vol.46 (16), p.3437-3440

2003

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Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors

Bioorganic & medicinal chemistry letters, 2004-11, Vol.14 (22), p.5543-5546

2004

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Discovery and Pharmacological Evaluation of Growth Hormone Secretagogue Receptor Antagonists

Journal of medicinal chemistry, 2006-07, Vol.49 (15), p.4459-4469

2006

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Discovery and Structure−Activity Relationship of Oxalylarylaminobenzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B

Journal of medicinal chemistry, 2003-05, Vol.46 (11), p.2093-2103

2003

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Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex

Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels

Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy

Fragment Screening and Assembly: A Highly Efficient Approach to a Selective and Cell Active Protein Tyrosine Phosphatase 1B Inhibitor

Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Behavior

CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16

Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer’s Disease: 2‑(3-Phenyl‑1H‑pyrazol-1-yl)-nicotinamides

Current status and future prospects for enabling chemistry technology in the drug discovery process [version 1; peer review: 2 approved]

Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo

Ligand association rates to the inner-variable-domain of a dual-variable-domain immunoglobulin are significantly impacted by linker design

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists

Analgesic potential of TRPV1 antagonists

Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Identification of a monoacid-Based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B

Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8

Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors

Selective Protein Tyrosine Phosphatase 1B Inhibitors: Targeting the Second Phosphotyrosine Binding Site with Non-Carboxylic Acid-Containing Ligands

Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors

Discovery and Pharmacological Evaluation of Growth Hormone Secretagogue Receptor Antagonists

1,4-Dihydroindeno[1,2-c]pyrazoles with Acetylenic Side Chains as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors with Low Affinity for the hERG Ion Channel

Discovery and Structure−Activity Relationship of Oxalylarylaminobenzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B

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