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Relationship between passive permeability, efflux, and predictability of clearance from in vitro metabolic intrinsic clearance

Drug metabolism and disposition, 2010-02, Vol.38 (2), p.223-231

2010

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Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2417-2430

2015

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Inhibition of Colony-Stimulating-Factor-1 Signaling in vivo with the Orally Bioavailable cFMS Kinase Inhibitor GW2580

Proceedings of the National Academy of Sciences - PNAS, 2005-11, Vol.102 (44), p.16078-16083

2005

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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement

ACS medicinal chemistry letters, 2016-12, Vol.7 (12), p.1062-1067

2016

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Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (12), p.4089-4093

2012

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Differential role of P-glycoprotein and breast cancer resistance protein in drug distribution into brain, CSF and peripheral nerve tissues in rats

Xenobiotica, 2015-06, Vol.45 (6), p.547-555

2015

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Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx‑V Peptide 5‑Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis

Journal of medicinal chemistry, 2018-11, Vol.61 (21), p.9500-9512

2018

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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.5990-6017

2017

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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.5969-5989

2017

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Dynamic modeling of cytochrome P450 inhibition in vitro: impact of inhibitor depletion on IC₅₀ shift

Drug metabolism and disposition, 2013-07, Vol.41 (7), p.1433

2013

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Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx‑1 Peptide–Antibody Conjugates

ACS chemical biology, 2017-09, Vol.12 (9), p.2427-2435

2017

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The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (15), p.3477-3485

2017

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Gender Effects on Rat Metabolism of AMG 900, an Orally Available Small Molecule Aurora Kinase Inhibitor

Drug metabolism letters, 2011-12, Vol.5 (4), p.290-297

2011

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Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds

Xenobiotica, 2012-09, Vol.42 (9), p.830-840

2012

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Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6307-6312

2009

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Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor

Journal of medicinal chemistry, 2010-09, Vol.53 (17), p.6368-6377

2010

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Bioactivation of Isothiazoles: Minimizing the Risk of Potential Toxicity in Drug Discovery

Chemical research in toxicology, 2010-11, Vol.23 (11), p.1743-1752

2010

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In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases

Xenobiotica, 2011-05, Vol.41 (5), p.400-408

2011

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Corrigendum to “Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors” [Bioorg. Med. Chem. Lett. 19 (2009) 6307]

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (2), p.773-773

2010

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Prediction of V ss from In Vitro Tissue-Binding Studies

Drug metabolism and disposition, 2010-01, Vol.38 (1), p.115-121

2010

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Dynamic Modeling of Cytochrome P450 Inhibition In Vitro: Impact of Inhibitor Depletion on IC 50 Shift

Drug metabolism and disposition, 2013-07, Vol.41 (7), p.1433-1441

2013

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Discovery of Tarantula Venom-Derived Na V 1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis

Journal of medicinal chemistry, 2018-11, Vol.61 (21), p.9500-9512

2018

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Relationship between passive permeability, efflux, and predictability of clearance from in vitro metabolic intrinsic clearance

Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors

Inhibition of Colony-Stimulating-Factor-1 Signaling in vivo with the Orally Bioavailable cFMS Kinase Inhibitor GW2580

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Differential role of P-glycoprotein and breast cancer resistance protein in drug distribution into brain, CSF and peripheral nerve tissues in rats

Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx‑V Peptide 5‑Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities

Discovery of N‑(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines

Dynamic modeling of cytochrome P450 inhibition in vitro: impact of inhibitor depletion on IC₅₀ shift

Discovery of (R)‑6-(1-(8-Fluoro-6-(1-methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)‑one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity

Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx‑1 Peptide–Antibody Conjugates

The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement

Gender Effects on Rat Metabolism of AMG 900, an Orally Available Small Molecule Aurora Kinase Inhibitor

Engineering Na V 1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics

Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor

Bioactivation of Isothiazoles: Minimizing the Risk of Potential Toxicity in Drug Discovery

In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases

Corrigendum to “Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors” [Bioorg. Med. Chem. Lett. 19 (2009) 6307]

Prediction of V ss from In Vitro Tissue-Binding Studies

Dynamic Modeling of Cytochrome P450 Inhibition In Vitro: Impact of Inhibitor Depletion on IC 50 Shift

Discovery of Tarantula Venom-Derived Na V 1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis

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