List of works - Emile G Plise

Antibody-Mediated Inhibition of Fibroblast Growth Factor 19 Results in Increased Bile Acids Synthesis and Ileal Malabsorption of Bile Acids in Cynomolgus Monkeys ⬇️

scientific article published on January 19, 2012

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

scientific article

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

scientific article published on 26 June 2019

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

scientific article published on 16 February 2016

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design

scientific article

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

scientific article

Evaluating the Utility of Canine Mdr1 Knockout Madin-Darby Canine Kidney I Cells in Permeability Screening and Efflux Substrate Determination

scientific article published on 10 October 2018

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile

scientific article published on 31 October 2016

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) ⬇️

scientific article published on March 25, 2011

Novel antibody-antibiotic conjugate eliminates intracellular S. aureus

scientific article

Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery

scientific article published on January 2014

Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human ⬇️

scientific article published on June 13, 2012

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human ⬇️

scientific article published on August 13, 2011

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

scientific article

Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

scientific article published on 3 June 2010

SAHA enhances synaptic function and plasticity in vitro but has limited brain availability in vivo and does not impact cognition

scientific article

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway ⬇️

scientific article published on September 15, 2010

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase ⬇️

scientific article published on August 19, 2010

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

scientific article

The Effects of Drug Metabolizing Enzyme Inhibitors on Hepatic Efflux and Uptake Transporters

scientific article published on 10 October 2017

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

scientific article published on 11 September 2012

Variability in P-glycoprotein inhibitory potency (IC₅₀) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria.

scientific article published on 25 April 2013

List of works by Emile G Plise

Antibody-Mediated Inhibition of Fibroblast Growth Factor 19 Results in Increased Bile Acids Synthesis and Ileal Malabsorption of Bile Acids in Cynomolgus Monkeys ⬇️

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

Evaluating the Utility of Canine Mdr1 Knockout Madin-Darby Canine Kidney I Cells in Permeability Screening and Efflux Substrate Determination

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) ⬇️

Novel antibody-antibiotic conjugate eliminates intracellular S. aureus

Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery

Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human ⬇️

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human ⬇️

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

SAHA enhances synaptic function and plasticity in vitro but has limited brain availability in vivo and does not impact cognition

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway ⬇️

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase ⬇️

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

The Effects of Drug Metabolizing Enzyme Inhibitors on Hepatic Efflux and Uptake Transporters

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

Variability in P-glycoprotein inhibitory potency (IC₅₀) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria.