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Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth

Molecular cancer therapeutics, 2016-10, Vol.15 (10), p.2344-2356

2016

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Principles of Kinase Allosteric Inhibition and Pocket Validation

Journal of medicinal chemistry, 2022-04, Vol.65 (7), p.5288-5299

2022

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Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes

Journal of medicinal chemistry, 2023-07, Vol.66 (14), p.9297-9312

2023

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The promise and peril of chemical probes

Nature chemical biology, 2015-08, Vol.11 (8), p.536-541

2015

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Binding Energy and Catalysis: The Implications for Transition-State Analogs and Catalytic Antibodies

Chemical reviews, 1997-08, Vol.97 (5), p.1281-1302

1997

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Which Small Molecule? Selecting Chemical Probes for Use in Cancer Research and Target Validation

Cancer discovery, 2023-10, Vol.13 (10), p.2150-2165

2023

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LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

ACS medicinal chemistry letters, 2018-07, Vol.9 (7), p.612-617

2018

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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2

Proceedings of the National Academy of Sciences - PNAS, 2024-02, Vol.121 (6), p.e2317756121-e2317756121

2024

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A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6

Journal of medicinal chemistry, 2021-04, Vol.64 (7), p.3697-3706

2021

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Complete Inhibition of Anisomycin and UV Radiation but Not Cytokine Induced JNK and p38 Activation by an Aryl-substituted Dihydropyrrolopyrazole Quinoline and Mixed Lineage Kinase 7 Small Interfering RNA

The Journal of biological chemistry, 2005-05, Vol.280 (19), p.19298-19305

2005

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Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

Cancer discovery, 2024-02, Vol.14 (2), p.240-257

2024

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Beyond PAINs: Chemotype Sensitivity of Protein Methyltransferases in Screens

ACS medicinal chemistry letters, 2016-02, Vol.7 (2), p.156-161

2016

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Structure-guided expansion of kinase fragment libraries driven by support vector machine models

Biochimica et biophysica acta, 2010-03, Vol.1804 (3), p.642-652

2010

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Acyclic Stereoselective Boron Alkylation Reactions for the Asymmetric Synthesis of β-Substituted α-Amino Acid Derivatives

Journal of the American Chemical Society, 2003-03, Vol.125 (9), p.2370-2371

2003

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Acyl Sulfonamide Anti-Proliferatives: Benzene Substituent Structure−Activity Relationships for a Novel Class of Antitumor Agents

Journal of medicinal chemistry, 2004-10, Vol.47 (22), p.5367-5380

2004

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Rationalizing Ring-Size Selectivity in Intramolecular Pd-Catalyzed Allylations of Resonance-Stabilized Carbanions

Organometallics, 2006-08, Vol.25 (17), p.4234-4234

2006

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Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives

Bioorganic & medicinal chemistry letters, 2005-02, Vol.15 (3), p.617-620

2005

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Quantum Chemical Investigation of Mechanisms of Silane Oxidation

Journal of the American Chemical Society, 2001-03, Vol.123 (9), p.1970-1976

2001

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Rationalizing Ring-Size Selectivity in Intramolecular Pd-Catalyzed Allylations of Resonance-Stabilized Carbanions

Organometallics, 2003-04, Vol.22 (9), p.1849-1855

2003

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Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators

Bioorganic & medicinal chemistry letters, 2002-10, Vol.12 (20), p.2875-2878

2002

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Computational Investigation of the Role of Fluoride in Tamao Oxidations

Chemistry : a European journal, 2002-11, Vol.8 (21), p.5043-5048

2002

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Silylacetic Esters: Enolate Reactions and Polyol Preparation

Journal of organic chemistry, 1998-04, Vol.63 (8), p.2761-2764

1998

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Erratum: Corrigendum: The promise and peril of chemical probes

Nature chemical biology, 2015-10, Vol.11 (11), p.887-887

2015

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Novel antiproliferative antitumor agents

Current opinion in drug discovery & development, 2005-09, Vol.8 (5), p.613

Mader, Mary M

2005

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Multistep electron transfer in palladium-catalyzed aerobic oxidations via a metal macrocycle quinone system

Journal of the American Chemical Society, 1990-06, Vol.112 (13), p.5160-5166

1990

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Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth

Principles of Kinase Allosteric Inhibition and Pocket Validation

Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes

The promise and peril of chemical probes

Binding Energy and Catalysis: The Implications for Transition-State Analogs and Catalytic Antibodies

Which Small Molecule? Selecting Chemical Probes for Use in Cancer Research and Target Validation

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2

A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6

Complete Inhibition of Anisomycin and UV Radiation but Not Cytokine Induced JNK and p38 Activation by an Aryl-substituted Dihydropyrrolopyrazole Quinoline and Mixed Lineage Kinase 7 Small Interfering RNA

Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

Beyond PAINs: Chemotype Sensitivity of Protein Methyltransferases in Screens

Structure-guided expansion of kinase fragment libraries driven by support vector machine models

Acyclic Stereoselective Boron Alkylation Reactions for the Asymmetric Synthesis of β-Substituted α-Amino Acid Derivatives

Acyl Sulfonamide Anti-Proliferatives: Benzene Substituent Structure−Activity Relationships for a Novel Class of Antitumor Agents

Rationalizing Ring-Size Selectivity in Intramolecular Pd-Catalyzed Allylations of Resonance-Stabilized Carbanions

Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives

Quantum Chemical Investigation of Mechanisms of Silane Oxidation

Rationalizing Ring-Size Selectivity in Intramolecular Pd-Catalyzed Allylations of Resonance-Stabilized Carbanions

Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators

Computational Investigation of the Role of Fluoride in Tamao Oxidations

Silylacetic Esters: Enolate Reactions and Polyol Preparation

Erratum: Corrigendum: The promise and peril of chemical probes

Novel antiproliferative antitumor agents

Multistep electron transfer in palladium-catalyzed aerobic oxidations via a metal macrocycle quinone system

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