PMID

Data

Article Title

Organization

Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.

Astrazeneca

Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.

Astrazeneca

Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro.

University of Oslo

Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.

Pfizer

Interaction of lapatinib with cytochrome P450 3A5.

National University of Singapore

Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.

Purdue University

Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptorß agonist in clinical trials for the treatment of dyslipidemia.

Madrigal Pharmaceuticals

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.

F. Hoffmann-La Roche

Wake-promoting agents: search for next generation modafinil: part IV.

Cephalon (France)

Wake-promoting agents: search for next generation modafinil: part II.

Cephalon

Imidazopyridines as selective CYP3A4 inhibitors.

The Scripps Research Institute

Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.

Novartis Institutes For Biomedical Research

Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis.

Nimbus Therapeutics

Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.

Pfizer

Unique Oxidative Metabolism of Bufalin Generates Two Reactive Metabolites That Strongly Inactivate Human Cytochrome P450 3A.

Shanghai University of Traditional Chinese Medicine

Enhancing monoamine oxidase B inhibitory activity via chiral fluorination: Structure-activity relationship, biological evaluation, and molecular docking study.

Central China Normal University

Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A

TBA

Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.

Cytokinetics

Discovery of

Zhejiang University

Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.

Anhui Medical University

Identification of 2,2-Dimethylbutanoic Acid (HST5040), a Clinical Development Candidate for the Treatment of Propionic Acidemia and Methylmalonic Acidemia.

Hemoshear Therapeutics

The Essential Medicinal Chemistry of Cannabidiol (CBD).

University of Minnesota

Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.

Haisco Pharmaceutical Group

Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.

University of Washington

Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.

University of Washington

Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.

Lindsley F. Kimball Research Institute

CN128: A New Orally Active Hydroxypyridinone Iron Chelator.

Zhejiang University

Discovery of new indole-based acylsulfonamide Na

Bristol-Myers Squibb Research and Development

Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.

Gwangju Institute of Science and Technology

Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.

St. Jude Children'S Research Hospital

Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.

Abide Therapeutics

Metabolically Stable tert-Butyl Replacement.

Novartis Institutes For Biomedical Research

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

Epichem

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.

Epichem

Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.

Keimyung University

Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.

Dart Neuroscience

Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.

Japan Tobacco

Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.

Mitsubishi Tanabe Pharma

Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.

Corcept Therapeutics