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Predicting Passive Permeability of Drug-like Molecules from Chemical Structure: Where Are We?

Molecular pharmaceutics, 2016-12, Vol.13 (12), p.4199-4208

2016

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502 Preclinical Pharmacokinetics and Efficacy Assessment of a Potent and Selective MEK Inhibitor, GDC-0623

European journal of cancer (1990), 2012-11, Vol.48, p.155-155

2012

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Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

Xenobiotica, 2009-11, Vol.39 (11), p.850-861

2009

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Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species

Xenobiotica, 2009-09, Vol.39 (9), p.700-709

2009

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

Journal of medicinal chemistry, 2011-04, Vol.54 (8), p.2592-2601

2011

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Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro- N -(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

Xenobiotica, 2009-09, p.90908054849067-12

2009

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

PloS one, 2013-07, Vol.8 (7), p.e69964

2013

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

ACS medicinal chemistry letters, 2016-04, Vol.7 (4), p.351-356

2016

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

Drug metabolism and disposition, 2016-12, Vol.44 (12), p.1881-1889

2016

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The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α

Journal of medicinal chemistry, 2012-09, Vol.55 (18), p.8007-8020

2012

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Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier

Clinical cancer research, 2012-11, Vol.18 (22), p.6239-6248

2012

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

Drug metabolism and disposition, 2013-07, Vol.41 (7), p.1347

2013

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

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2760-2779

2016

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A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C

PloS one, 2012-01, Vol.7 (1), p.e30376

2012

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

ACS medicinal chemistry letters, 2017-01, Vol.8 (1), p.84-89

2017

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

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (22), p.6748-6753

2010

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Predicting Passive Permeability of Drug-like Molecules from Chemical Structure: Where Are We?

502 Preclinical Pharmacokinetics and Efficacy Assessment of a Potent and Selective MEK Inhibitor, GDC-0623

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species

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

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro- N -(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

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

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

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

The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α

Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier

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

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

A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C

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

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

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