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Papers authored by Humphreys WG

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Bioactivation of coumarin in rat olfactory mucosal microsomes: Detection of protein covalent binding and identification of reactive intermediates through analysis of glutathione adducts.

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Zhuo X, Zhao W, Zheng J, Humphreys WG, Shu YZ, and Zhu M

Chemico-biological interactions 181(2):227-35, 2009 Oct 7 - Who cited this? | PubMed ID: 19576871 | Fulltext

The Pneumotoxin 3-Methylindole Is a Substrate and a Mechanism-Based Inactivator of CYP2A13, a Human Cytochrome P450 Enzyme Preferentially Expressed in the Respiratory Tract.

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D'Agostino J, Zhuo X, Shadid M, Morgan DG, Zhang X, Humphreys WG, Shu YZ, Yost GS, and Ding X

Drug metabolism and disposition: the biological fate of chemicals 37(10):2018-27, 2009 Oct - Who cited this? | PubMed ID: 19608696 | Fulltext

Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans.

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Zhang D, He K, Raghavan N, Wang L, Mitroka J, Maxwell BD, Knabb RM, Frost C, Schuster A, Hao F, Gu Z, Humphreys WG, and Grossman SJ

Drug metabolism and disposition: the biological fate of chemicals 37(8):1738-48, 2009 Aug - Who cited this? | PubMed ID: 19420130 | Fulltext

Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.

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Fura A, Khanna A, Vyas V, Koplowitz B, Chang SY, Caporuscio C, Boulton DW, Christopher LJ, Chadwick KD, Hamann LG, Humphreys WG, and Kirby M

Drug metabolism and disposition: the biological fate of chemicals 37(6):1164-71, 2009 Jun - Who cited this? | PubMed ID: 19251818 | Fulltext

Metabolism and excretion of an oral taxane analog, [14C]3'-tert-butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-N-debenzoyl-4-O-methoxy-paclitaxel (BMS-275183), in rats and dogs.

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Ly VT, Caceres-Cortes J, Zhang D, Humphreys WG, Ekhato IV, Everett D, and Cömezoğlu SN

Drug metabolism and disposition: the biological fate of chemicals 37(5):1115-28, 2009 May - Who cited this? | PubMed ID: 19196843 | Fulltext

Sulfation of o-demethyl apixaban: enzyme identification and species comparison.

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Wang L, Raghavan N, He K, Luettgen JM, Humphreys WG, Knabb RM, Pinto DJ, and Zhang D

Drug metabolism and disposition: the biological fate of chemicals 37(4):802-8, 2009 Apr - Who cited this? | PubMed ID: 19131519 | Fulltext

CYP3A4-mediated ester cleavage as the major metabolic pathway of the oral taxane 3'-tert-butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel (BMS-275183).

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Zhang D, Ly VT, Lago M, Tian Y, Gan J, Humphreys WG, and Cömezoglu SN

Drug metabolism and disposition: the biological fate of chemicals 37(4):710-8, 2009 Apr - Who cited this? | PubMed ID: 19158314 | Fulltext

Algorithm for Thorough Background Subtraction of High-Resolution LC/MS Data: Application to Obtain Clean Product Ion Spectra from Nonselective Collision-Induced Dissociation Experiments.

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Zhang H, Grubb M, Wu W, Josephs J, and Humphreys WG

Analytical chemistry 81(7):2695-700, 2009 Apr 1 - Who cited this? | PubMed ID: 19254033 | Fulltext

In vitro screening of 50 highly prescribed drugs for thiol adduct formation--comparison of potential for drug-induced toxicity and extent of adduct formation.

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Gan J, Ruan Q, He B, Zhu M, Shyu WC, and Humphreys WG

Chemical research in toxicology 22(4):690-8, 2009 Apr - Who cited this? | PubMed ID: 19253935 | Fulltext

Apixaban metabolism and pharmacokinetics after oral administration to humans.

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Raghavan N, Frost CE, Yu Z, He K, Zhang H, Humphreys WG, Pinto D, Chen S, Bonacorsi S, Wong PC, and Zhang D

Drug metabolism and disposition: the biological fate of chemicals 37(1):74-81, 2009 Jan - Who cited this? | PubMed ID: 18832478 | Fulltext

Rapid screening and characterization of drug metabolites using a multiple ion monitoring-dependent MS/MS acquisition method on a hybrid triple quadrupole-linear ion trap mass spectrometer.

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Yao M, Ma L, Humphreys WG, and Zhu M

Journal of mass spectrometry : JMS 43(10):1364-75, 2008 Oct - Who cited this? | PubMed ID: 18416441 | Fulltext

Lacteal Excretion, Fetal and Maternal Tissue Distribution of Dasatinib in Rats.

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He K, Lago MW, Iyer RA, Shyu WC, Humphreys WG, and Christopher LJ

Drug metabolism and disposition: the biological fate of chemicals, 2008 Sep 11 - Who cited this? | PubMed ID: 18787054 | Fulltext

Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

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Ellsworth BA, Meng W, Patel M, Girotra RN, Wu G, Sher PM, Hagan DL, Obermeier MT, Humphreys WG, Robertson JG, Wang A, Han S, Waldron TL, Morgan NN, Whaley JM, and Washburn WN

Bioorganic & medicinal chemistry letters 18(17):4770-3, 2008 Sep 1 - Who cited this? | PubMed ID: 18707880 | Fulltext

(d)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: Synthesis and incorporation into the growth hormone secretagogues.

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Li J, Chen SY, Murphy BJ, Flynn N, Seethala R, Slusarchyk D, Yan M, Sleph P, Zhang H, Humphreys WG, Ewing WR, Robl JA, Gordon D, and Tino JA

Bioorganic & medicinal chemistry letters 18(14):4072-4, 2008 Jul 15 - Who cited this? | PubMed ID: 18554903 | Fulltext

Biotransformation of [14C]dasatinib: in vitro studies in rat, monkey, and human and disposition after administration to rats and monkeys.

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Christopher LJ, Cui D, Li W, Barros A, Arora VK, Zhang H, Wang L, Zhang D, Manning JA, He K, Fletcher AM, Ogan M, Lago M, Bonacorsi SJ, Humphreys WG, and Iyer RA

Drug metabolism and disposition: the biological fate of chemicals 36(7):1341, 2008 Jul - Who cited this? | PubMed ID: 18420785 | Fulltext

Metabolism and disposition of dasatinib after oral administration to humans.

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Christopher LJ, Cui D, Wu C, Luo R, Manning JA, Bonacorsi SJ, Lago M, Allentoff A, Lee FY, McCann B, Galbraith S, Reitberg DP, He K, Barros A, Blackwood-Chirchir A, Humphreys WG,

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Drug metabolism and disposition: the biological fate of chemicals 36(7):1357, 2008 Jul - Who cited this? | PubMed ID: 18420784 | Fulltext

IDENTIFICATION OF THE HUMAN ENZYMES INVOLVED IN THE OXIDATIVE METABOLISM OF DASATINIB. AN EFFECTIVE APPROACH FOR DETERMINING METABOLITE FORMATION KINETICS.

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Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, and Zhang D

Drug metabolism and disposition: the biological fate of chemicals, 2008 Jun 12 - Who cited this? | PubMed ID: 18556438 | Fulltext

The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of ixabepilone: a first in class epothilone B analogue in late-phase clinical development.

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Goel S, Cohen M, Cömezoglu SN, Perrin L, André F, Jayabalan D, Iacono L, Comprelli A, Ly VT, Zhang D, Xu C, Humphreys WG, McDaid H, Goldberg G, Horwitz SB, and Mani S

Clinical cancer research : an official journal of the American Association for Cancer Research 14(9):2701-9, 2008 May 1 - Who cited this? | PubMed ID: 18451235 | Fulltext

Metabolite generation via microbial biotransformations with Actinomycetes: rapid screening for active strains and biosynthesis of important human metabolites of two development-stage compounds, 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-.

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Li W, Josephs JL, Skiles GL, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 36(4):721, 2008 Apr - Who cited this? | PubMed ID: 18227141 | Fulltext

Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

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Hernández AS, Swartz SG, Slusarchyk D, Yan M, Seethala RK, Sleph P, Grover G, Dickinson K, Giupponi L, Harper TW, Humphreys WG, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA,

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Bioorganic & medicinal chemistry letters 18(6):2067-72, 2008 Mar 15 - Who cited this? | PubMed ID: 18282707 | Fulltext

Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.

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Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P,

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Bioorganic & medicinal chemistry letters 18(6):1825-9, 2008 Mar 15 - Who cited this? | PubMed ID: 18295486 | Fulltext

Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes.

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Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR,

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Journal of medicinal chemistry 51(5):1145-9, 2008 Mar 13 - Who cited this? | PubMed ID: 18260618 | Fulltext

An integrated method for metabolite detection and identification using a linear ion trap/Orbitrap mass spectrometer and multiple data processing techniques: application to indinavir metabolite detection.

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Ruan Q, Peterman S, Szewc MA, Ma L, Cui D, Humphreys WG, and Zhu M

Journal of mass spectrometry : JMS 43(2):251-61, 2008 Feb - Who cited this? | PubMed ID: 17968853 | Fulltext

Characterization of the UDP Glucuronosyltransferase Activity of Human Liver Microsomes Genotyped for the UGT1A1*28 Polymorphism.

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Zhang D, Zhang D, Cui D, Gambardella J, Ma L, Barros A, Wang L, Fu Y, Rahematpura S, Nielsen J, Donegan M, Zhang H, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 35(12):2270-80, 2007 Dec - Who cited this? | PubMed ID: 17898154 | Fulltext

LC-MS/MS-based approach for obtaining exposure estimates of metabolites in early clinical trials using radioactive metabolites as reference standards.

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Zhang D, Raghavan N, Chando T, Gambardella J, Fu Y, Zhang D, Unger SE, and Humphreys WG

Drug metabolism letters 1(4):293-8, 2007 Dec - Who cited this? | PubMed ID: 19356058 | Fulltext

Discovery of a Tetrazole-Based Growth Hormone Secretagogue: 4-(Hydroxybutyl)carbamic Acid 2-{5-[1-(2-Amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl Ester (BMS-317180).

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Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P,

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Journal of medicinal chemistry 50(24):5890-3, 2007 Nov 29 - Who cited this? | PubMed ID: 17973363 | Fulltext

Detection and structural characterization of glutathione-trapped reactive metabolites using liquid chromatography-high-resolution mass spectrometry and mass defect filtering.

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Zhu M, Ma L, Zhang H, and Humphreys WG

Analytical chemistry 79(21):8333-41, 2007 Nov 1 - Who cited this? | PubMed ID: 17918967 | Fulltext

Development and full validation of six inhibition assays for five major cytochrome P450 enzymes in human liver microsomes using an automated 96-well microplate incubation format and LC-MS/MS analysis.

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Yao M, Zhu M, Sinz MW, Zhang H, Humphreys WG, Rodrigues AD, and Dai R

Journal of pharmaceutical and biomedical analysis 44(1):211-23, 2007 May 9 - Who cited this? | PubMed ID: 17418993 | Fulltext

Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys.

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Zhang H, Zhang D, Li W, Yao M, D'Arienzo C, Li YX, Ewing WR, Gu Z, Zhu Y, Murugesan N, Shyu WC, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 35(5):795, 2007 May - Who cited this? | PubMed ID: 17303626 | Fulltext

Screening and identification of GSH-trapped reactive metabolites using hybrid triple quadruple linear ion trap mass spectrometry.

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Zheng J, Ma L, Xin B, Olah T, Humphreys WG, and Zhu M

Chemical research in toxicology 20(5):757-66, 2007 May - Who cited this? | PubMed ID: 17402749 | Fulltext

Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.

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Zhang D, Wang L, Raghavan N, Zhang H, Li W, Cheng PT, Yao M, Zhang L, Zhu M, Bonacorsi S, Yeola S, Mitroka J, Hariharan N, Hosagrahara V, Chandrasena G, Shyu WC,

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Drug metabolism and disposition: the biological fate of chemicals 35(1):150, 2007 Jan - Who cited this? | PubMed ID: 17062777 | Fulltext

Involvement of multiple cytochrome P450 and UDP-glucuronosyltransferase enzymes in the in vitro metabolism of muraglitazar.

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Zhang D, Wang L, Chandrasena G, Ma L, Zhu M, Zhang H, Davis CD, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 35(1):139-49, 2007 Jan - Who cited this? | PubMed ID: 17062778 | Fulltext

Pharmacokinetics of muraglitazar (BMS-298585), a dual peroxisome proliferator-activated receptors (PPAR) alpha and gamma activator, in mice, rats, dogs, and monkeys.

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Hosagrahara VP, Chandrasena G, Chang SY, Koplowitz B, Hariharan N, Cheng PT, and Humphreys WG

Xenobiotica; the fate of foreign compounds in biological systems 36(12):1227-38, 2006 Dec - Who cited this? | PubMed ID: 17162469 | Fulltext

Safety assessment of drug metabolites: Characterization of chemically stable metabolites.

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Humphreys WG and Unger SE

Chemical research in toxicology 19(12):1564-9, 2006 Dec - Who cited this? | PubMed ID: 17173369 | Fulltext

Detection and characterization of metabolites in biological matrices using mass defect filtering of liquid chromatography/high resolution mass spectrometry data.

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Zhu M, Ma L, Zhang D, Ray K, Zhao W, Humphreys WG, Skiles G, Sanders M, and Zhang H

Drug metabolism and disposition: the biological fate of chemicals 34(10):1722-33, 2006 Oct - Who cited this? | PubMed ID: 16815965 | Fulltext

Biotransformation of carbon-14-labeled muraglitazar in male mice: interspecies difference in metabolic pathways leading to unique metabolites.

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Li W, Zhang D, Wang L, Zhang H, Cheng PT, Zhang D, Everett DW, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 34(5):807, 2006 May - Who cited this? | PubMed ID: 16467134 | Fulltext

Glucuronidation as a major metabolic clearance pathway of 14c-labeled muraglitazar in humans: metabolic profiles in subjects with or without bile collection.

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Wang L, Zhang D, Swaminathan A, Xue Y, Cheng PT, Wu S, Mosqueda-Garcia R, Aurang C, Everett DW, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 34(3):427-39, 2006 Mar - Who cited this? | PubMed ID: 16381667 | Fulltext

Structural elucidation of human oxidative metabolites of muraglitazar: use of microbial bioreactors in the biosynthesis of metabolite standards.

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Zhang D, Zhang H, Aranibar N, Hanson R, Huang Y, Cheng PT, Wu S, Bonacorsi S, Zhu M, Swaminathan A, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 34(2):267-80, 2006 Feb - Who cited this? | PubMed ID: 16280454 | Fulltext

In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation.

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Zhang D, Chando TJ, Everett DW, Patten CJ, Dehal SS, and Humphreys WG

Drug metabolism and disposition: the biological fate of chemicals 33(11):1729-39, 2005 Nov - Who cited this? | PubMed ID: 16118329 | Fulltext

Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites.

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Gan J, Harper TW, Hsueh MM, Qu Q, and Humphreys WG

Chemical research in toxicology 18(5):896-903, 2005 May - Who cited this? | PubMed ID: 15892584 | Fulltext

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

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Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R,

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Journal of medicinal chemistry 48(6):2248-50, 2005 Mar 24 - Who cited this? | PubMed ID: 15771468 | Fulltext

Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.

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Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R,

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Journal of medicinal chemistry 48(1):171-9, 2005 Jan 13 - Who cited this? | PubMed ID: 15634011 | Fulltext

CYP3A4 induction by xenobiotics: biochemistry, experimental methods and impact on drug discovery and development.

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Luo G, Guenthner T, Gan LS, and Humphreys WG

Current drug metabolism 5(6):483-505, 2004 Dec - Who cited this? | PubMed ID: 15578943 | Fulltext

Discovering drugs through biological transformation: role of pharmacologically active metabolites in drug discovery.

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Fura A, Shu YZ, Zhu M, Hanson RL, Roongta V, and Humphreys WG

Journal of medicinal chemistry 47(18):4339-51, 2004 Aug 26 - Who cited this? | PubMed ID: 15317447 | Fulltext

The use of radiolabeled compounds for ADME studies in discovery and exploratory development.

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Marathe PH, Shyu WC, and Humphreys WG

Current pharmaceutical design 10(24):2991-3008, 2004 - Who cited this? | PubMed ID: 15379664 | Fulltext

Information provided to patients undergoing gastroscopy procedures.

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Thompson K, Melby V, Parahoo K, Ridley T, and Humphreys WG

Journal of clinical nursing 12(6):899-911, 2003 Nov - Who cited this? | PubMed ID: 14632983 | Fulltext

Application of structure-metabolism relationships in the identification of a selective endothelin A antagonist, BMS-193884, with favourable pharmacokinetic properties.

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Humphreys WG, Obermeier MT, Barrish JC, Chong S, Marino AM, Murugesan N, Wang-Iverson D, and Morrison RA

Xenobiotica; the fate of foreign compounds in biological systems 33(11):1109-23, 2003 Nov - Who cited this? | PubMed ID: 14660175 | Fulltext

Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.

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Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S,

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Journal of medicinal chemistry 46(1):125-37, 2003 Jan 2 - Who cited this? | PubMed ID: 12502366 | Fulltext

Oxidative activation of acylguanidine prodrugs: intestinal presystemic activation in rats limits absorption and can be inhibited by co-administration of ketoconazole.

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Humphreys WG, Obermeier MT, Chong S, Kimball SD, Das J, Chen P, Moquin R, Han WC, Gedamke R, White RE, and Morrison RA

Xenobiotica; the fate of foreign compounds in biological systems 33(1):93-106, 2003 Jan - Who cited this? | PubMed ID: 12519697 | Fulltext

Pharmacokinetics and metabolism of endothelin receptor antagonist: contribution of kidneys in the overall in vivo N-demethylation.

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Chong S, Obermeier M, and Humphreys WG

Archives of pharmacal research 26(1):89-94, 2003 Jan - Who cited this? | PubMed ID: 12568365 | Fulltext

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