THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL

Angela C. Doran, R. Scott Obach, Bill J. Smith, +37

Drug Metabolism and Disposition

DEVELOPMENT OF A COMPUTATIONAL APPROACH TO PREDICT BLOOD-BRAIN BARRIER PERMEABILITY

Xingrong Liu, Meihua Tu, Rebecca S. Kelly, +2

Drug Metabolism and Disposition

Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing

Romain Rouet, Benjamin A. Thuma, Marc D. Roy, +24

Journal of the American Chemical Society

Molecular BiologyAsialoglycoprotein Receptor LigandsGenome EngineeringCrisprAntisense Therapy +15

Are 2D fingerprints still valuable for drug discovery?

Kaifu Gao, Duc Duy Nguyen, Vishnu Sresht, +3

Physical Chemistry Chemical Physics

Molecular FingerprintsDrug TargetEngineeringHit IdentificationMicroscopy +17

Generative Network Complex for the Automated Generation of Drug-like Molecules

Kaifu Gao, Duc Duy Nguyen, Meihua Tu, +1

Journal of Chemical Information and Modeling

Drug TargetNew Drug CandidatesEngineeringGenerative Network ComplexSynthetic Circuit +18

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1<i>H</i>-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Kimberly O. Cameron, Daniel W. Kung, Amit S. Kalgutkar, +30

Journal of Medicinal Chemistry

Renal InflammationPharmacotherapyInsulin SignalingMolecular PharmacologyMedicinal Chemistry +17

Discovery of (<i>S</i>)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1<i>H</i>-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus

Jeffrey A. Pfefferkorn, Angel Guzmán-Pérez, John Litchfield, +41

Journal of Medicinal Chemistry

Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors

Thomas A. Chappie, John M. Humphrey, Martin P. Allen, +11

Journal of Medicinal Chemistry

Combinatorial Chemistry6,7-Dimethoxy-4-pyrrolidylquinazoline Pde10a InhibitorsPharmacotherapyAryl EtherHeterocycle Chemistry +14

Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor

Carlos Sanhueza, Michael M. Baksh, Benjamin A. Thuma, +21

Journal of the American Chemical Society

Drug TargetMedicinal ChemistryAsialoglycoprotein ReceptorBiochemistryCompact Ligand +17

Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle

Jeffrey A. Pfefferkorn, Jihong Lou, Martha L. Minich, +14

Bioorganic & Medicinal Chemistry Letters

Unique Metabolic LiabilityBiochemistryMedicineMechanism Of ActionGlucokinase Activators +8