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Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Icahn School of Medicine At Mount Sinai

Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7.

Icahn School of Medicine At Mount Sinai

Non-Substrate Based, Small Molecule Inhibitors of the Human Isoprenylcysteine Carboxyl Methyltransferase.

Icahn School of Medicine At Mount Sinai

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai

Selective inhibitors of protein methyltransferases.

Icahn School of Medicine At Mount Sinai

Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).

Icahn School of Medicine At Mount Sinai

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.

Icahn School of Medicine At Mount Sinai

Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.

Icahn School of Medicine At Mount Sinai

Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer.

Icahn School of Medicine At Mount Sinai

DYRK1A Inhibitors as Potential Therapeutics for β-Cell Regeneration for Diabetes.

Icahn School of Medicine At Mount Sinai

Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.

Icahn School of Medicine At Mount Sinai

Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos.

Icahn School of Medicine At Mount Sinai

Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.

Icahn School of Medicine At Mount Sinai

Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.

Icahn School of Medicine At Mount Sinai

Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.

Icahn School of Medicine At Mount Sinai

Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies.

Icahn School of Medicine At Mount Sinai

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

Icahn School of Medicine At Mount Sinai

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

Icahn School of Medicine At Mount Sinai

Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.

Icahn School of Medicine At Mount Sinai

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

Icahn School of Medicine At Mount Sinai

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

Icahn School of Medicine At Mount Sinai

Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68).

Icahn School of Medicine At Mount Sinai

D

Icahn School of Medicine At Mount Sinai

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.

Icahn School of Medicine At Mount Sinai

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Icahn School of Medicine At Mount Sinai

Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.

Icahn School of Medicine At Mount Sinai

Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.

Icahn School of Medicine At Mount Sinai

Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader.

Icahn School of Medicine At Mount Sinai

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

Icahn School of Medicine At Mount Sinai

Structure-activity relationship studies of SETD8 inhibitors.

Icahn School of Medicine At Mount Sinai

Design, synthesis, and biological evaluation of (E)-N-aryl-2-arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents.

Icahn School of Medicine At Mount Sinai

Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity.

Icahn School of Medicine At Mount Sinai

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).

Icahn School of Medicine At Mount Sinai

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.

Icahn School of Medicine At Mount Sinai

Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).

Icahn School of Medicine At Mount Sinai

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

Icahn School of Medicine At Mount Sinai

IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AND THEIR USE IN THERAPY

Imperial College Innovations Limited; MyricX Pharma Limited

IRAK degraders and uses thereof

Dana-Farber Cancer Institute

Sulfonyl piperidine derivatives and their use for treating prokineticin mediated diseases

Takeda Pharmaceutical

In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.

University of Innsbruck