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Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors

Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1789-1811

2011

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Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor

Drug metabolism and disposition, 2003-11, Vol.31 (11), p.1352-1360

2003

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Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans

The Journal of pharmacology and experimental therapeutics, 2010-01, Vol.332 (1), p.17

2010

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Pyrene·Pyrene Complexes at the Active Site of Cytochrome P450 3A4: Evidence for a Multiple Substrate Binding Site

Journal of the American Chemical Society, 2002-10, Vol.124 (40), p.11866-11867

2002

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Structural characterization of novel adenine dinucleotide phosphate conjugates of imatinib in incubations with rat and human liver microsomes

Drug metabolism and disposition, 2008-12, Vol.36 (12), p.2414-2418

2008

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Solvent effect on cDNA-expressed human sulfotransferase (SULT) activities in vitro

Drug metabolism and disposition, 2003-11, Vol.31 (11), p.1300-1305

2003

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Triazolam substrate inhibition: evidence of competition for heme-bound reactive oxygen within the CYP3A4 active site

Drug metabolism and disposition, 2001-01, Vol.29 (1), p.70

2001

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A Refined 3-Dimensional QSAR of Cytochrome P450 2C9: Computational Predictions of Drug Interactions

Journal of medicinal chemistry, 2000-07, Vol.43 (15), p.2789-2796

2000

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Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS

ACS medicinal chemistry letters, 2011-02, Vol.2 (2), p.97-101

2011

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Phase I and Biomarker Study of the Wnt Pathway Modulator DKN-01 in Combination with Gemcitabine/Cisplatin in Advanced Biliary Tract Cancer

Clinical cancer research, 2020-12, Vol.26 (23), p.6158-6167

2020

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Covalent Alteration of the CYP3A4 Active Site: Evidence for Multiple Substrate Binding Domains

Archives of biochemistry and biophysics, 2001-07, Vol.391 (1), p.49-55

2001

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Heterotropic modulation of sulfotransferase 2A1 activity by celecoxib: product ratio switching of ethynylestradiol sulfation

Drug metabolism and disposition, 2004-11, Vol.32 (11), p.1260-1264

2004

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Cytochrome P450 2C8 (CYP2C8)-mediated hydroxylation of an endothelin ETA receptor antagonist in human liver microsomes

Drug metabolism and disposition, 2004-05, Vol.32 (5), p.473

2004

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Mechanism-Based Inactivation of Cytochrome P450 2B1 by 7-Ethynylcoumarin: Verification of Apo-P450 Adduction by Electrospray Ion Trap Mass Spectrometry

Chemical research in toxicology, 2000-04, Vol.13 (4), p.262-270

2000

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Catalytic turnover of pyrene by CYP3A4: evidence that cytochrome b5 directly induces positive cooperativity

Archives of biochemistry and biophysics, 2005-06, Vol.438 (1), p.21-28

2005

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HETEROTROPIC MODULATION OF SULFOTRANSFERASE 2A1 ACTIVITY BY CELECOXIB: PRODUCT RATIO SWITCHING OF ETHYNYLESTRADIOL SULFATION

Drug metabolism and disposition, 2004-11, Vol.32 (11), p.1260-1264

2004

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Sulfotransferase 1E1 is a low km isoform mediating the 3-O-sulfation of ethinyl estradiol

Drug metabolism and disposition, 2004-11, Vol.32 (11), p.1299

2004

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Catalytic turnover of pyrene by CYP3A4: Evidence that cytochrome b 5 directly induces positive cooperativity

Archives of biochemistry and biophysics, 2005-06, Vol.438 (1), p.21-28

2005

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Benzodiazepine Binding Site Occupancy by the Novel GABA A Receptor Subtype-Selective Drug 7-(1,1-Dimethylethyl)-6-(2-ethyl- 2H -1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3- b ]pyridazine (TPA023) in Rats, Primates, and Humans

The Journal of pharmacology and experimental therapeutics, 2010-01, Vol.332 (1), p.17-25

2010

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Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5

ACS medicinal chemistry letters, 2011-02, Vol.2 (2), p.107-112

2011

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SULFOTRANSFERASE 1E1 IS A LOW K M ISOFORM MEDIATING THE 3- O -SULFATION OF ETHINYL ESTRADIOL

Drug metabolism and disposition, 2004-11, Vol.32 (11), p.1299-1303

2004

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Topological alteration of the CYP3A4 active site by the divalent cation Mg(2+)

Drug metabolism and disposition, 2000-10, Vol.28 (10), p.1198

2000

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Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P1 agonists with in vivo lymphocyte-depleting activity

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.628-633

2012

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Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors

Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor

Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans

Pyrene·Pyrene Complexes at the Active Site of Cytochrome P450 3A4: Evidence for a Multiple Substrate Binding Site

Naphthamides as Novel and Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Design, Synthesis, and Evaluation

Structural characterization of novel adenine dinucleotide phosphate conjugates of imatinib in incubations with rat and human liver microsomes

Solvent effect on cDNA-expressed human sulfotransferase (SULT) activities in vitro

Triazolam substrate inhibition: evidence of competition for heme-bound reactive oxygen within the CYP3A4 active site

A Refined 3-Dimensional QSAR of Cytochrome P450 2C9: Computational Predictions of Drug Interactions

Evaluation of a Series of Naphthamides as Potent, Orally Active Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitors

Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS

Phase I and Biomarker Study of the Wnt Pathway Modulator DKN-01 in Combination with Gemcitabine/Cisplatin in Advanced Biliary Tract Cancer

Covalent Alteration of the CYP3A4 Active Site: Evidence for Multiple Substrate Binding Domains

Heterotropic modulation of sulfotransferase 2A1 activity by celecoxib: product ratio switching of ethynylestradiol sulfation

Cytochrome P450 2C8 (CYP2C8)-mediated hydroxylation of an endothelin ETA receptor antagonist in human liver microsomes

Mechanism-Based Inactivation of Cytochrome P450 2B1 by 7-Ethynylcoumarin: Verification of Apo-P450 Adduction by Electrospray Ion Trap Mass Spectrometry

Catalytic turnover of pyrene by CYP3A4: evidence that cytochrome b5 directly induces positive cooperativity

HETEROTROPIC MODULATION OF SULFOTRANSFERASE 2A1 ACTIVITY BY CELECOXIB: PRODUCT RATIO SWITCHING OF ETHYNYLESTRADIOL SULFATION

Sulfotransferase 1E1 is a low km isoform mediating the 3-O-sulfation of ethinyl estradiol

Catalytic turnover of pyrene by CYP3A4: Evidence that cytochrome b 5 directly induces positive cooperativity

Benzodiazepine Binding Site Occupancy by the Novel GABA A Receptor Subtype-Selective Drug 7-(1,1-Dimethylethyl)-6-(2-ethyl- 2H -1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3- b ]pyridazine (TPA023) in Rats, Primates, and Humans

Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5

SULFOTRANSFERASE 1E1 IS A LOW K M ISOFORM MEDIATING THE 3- O -SULFATION OF ETHINYL ESTRADIOL

Topological alteration of the CYP3A4 active site by the divalent cation Mg(2+)

Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P1 agonists with in vivo lymphocyte-depleting activity

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