| Rank |
Title |
Journal |
Year |
PubWeight™‹?› |
|
1
|
Apixaban metabolism and pharmacokinetics after oral administration to humans.
|
Drug Metab Dispos
|
2008
|
2.45
|
|
2
|
In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation.
|
Drug Metab Dispos
|
2005
|
2.19
|
|
3
|
Metabolism and disposition of dasatinib after oral administration to humans.
|
Drug Metab Dispos
|
2008
|
1.74
|
|
4
|
Role of CYP2A5 in the clearance of nicotine and cotinine: insights from studies on a Cyp2a5-null mouse model.
|
J Pharmacol Exp Ther
|
2009
|
1.29
|
|
5
|
In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies.
|
Drug Metab Dispos
|
2009
|
1.26
|
|
6
|
Detection and characterization of metabolites in biological matrices using mass defect filtering of liquid chromatography/high resolution mass spectrometry data.
|
Drug Metab Dispos
|
2006
|
1.15
|
|
7
|
CYP3A4 induction by xenobiotics: biochemistry, experimental methods and impact on drug discovery and development.
|
Curr Drug Metab
|
2004
|
1.13
|
|
8
|
Drug metabolite profiling and identification by high-resolution mass spectrometry.
|
J Biol Chem
|
2011
|
1.11
|
|
9
|
Discovering drugs through biological transformation: role of pharmacologically active metabolites in drug discovery.
|
J Med Chem
|
2004
|
1.02
|
|
10
|
Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.
|
Drug Metab Dispos
|
2009
|
1.02
|
|
11
|
Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics.
|
Drug Metab Dispos
|
2008
|
1.01
|
|
12
|
Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans.
|
Drug Metab Dispos
|
2009
|
0.95
|
|
13
|
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.
|
J Mass Spectrom
|
2008
|
0.92
|
|
14
|
Characterization of the UDP glucuronosyltransferase activity of human liver microsomes genotyped for the UGT1A1*28 polymorphism.
|
Drug Metab Dispos
|
2007
|
0.92
|
|
15
|
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.
|
Drug Metab Dispos
|
2009
|
0.91
|
|
16
|
Overcoming bioanalytical challenges in an Onglyza(®) intravenous [(14)C]microdose absolute bioavailability study with accelerator MS.
|
Bioanalysis
|
2012
|
0.91
|
|
17
|
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.
|
J Med Chem
|
2005
|
0.90
|
|
18
|
Characterization of efflux transporters involved in distribution and disposition of apixaban.
|
Drug Metab Dispos
|
2013
|
0.90
|
|
19
|
Tissue distribution and elimination of [14C]apixaban in rats.
|
Drug Metab Dispos
|
2010
|
0.90
|
|
20
|
Sulfation of o-demethyl apixaban: enzyme identification and species comparison.
|
Drug Metab Dispos
|
2009
|
0.90
|
|
21
|
Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.
|
Chem Res Toxicol
|
2012
|
0.89
|
|
22
|
Detection and structural characterization of glutathione-trapped reactive metabolites using liquid chromatography-high-resolution mass spectrometry and mass defect filtering.
|
Anal Chem
|
2007
|
0.88
|
|
23
|
Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats.
|
Drug Metab Dispos
|
2013
|
0.88
|
|
24
|
The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of ixabepilone: a first in class epothilone B analogue in late-phase clinical development.
|
Clin Cancer Res
|
2008
|
0.87
|
|
25
|
Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites.
|
Chem Res Toxicol
|
2005
|
0.86
|
|
26
|
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human.
|
Drug Metab Dispos
|
2012
|
0.86
|
|
27
|
Biotransformation of [14C]dasatinib: in vitro studies in rat, monkey, and human and disposition after administration to rats and monkeys.
|
Drug Metab Dispos
|
2008
|
0.84
|
|
28
|
Screening and identification of GSH-trapped reactive metabolites using hybrid triple quadruple linear ion trap mass spectrometry.
|
Chem Res Toxicol
|
2007
|
0.84
|
|
29
|
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.
|
J Mass Spectrom
|
2008
|
0.84
|
|
30
|
Involvement of multiple cytochrome P450 and UDP-glucuronosyltransferase enzymes in the in vitro metabolism of muraglitazar.
|
Drug Metab Dispos
|
2006
|
0.83
|
|
31
|
LC-MS/MS-based approach for obtaining exposure estimates of metabolites in early clinical trials using radioactive metabolites as reference standards.
|
Drug Metab Lett
|
2007
|
0.83
|
|
32
|
Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
|
J Med Chem
|
2005
|
0.83
|
|
33
|
Quantitative estimation of circulating metabolites without synthetic standards by ultra-high-performance liquid chromatography/high resolution accurate mass spectrometry in combination with UV correction.
|
Rapid Commun Mass Spectrom
|
2011
|
0.81
|
|
34
|
Structural elucidation of human oxidative metabolites of muraglitazar: use of microbial bioreactors in the biosynthesis of metabolite standards.
|
Drug Metab Dispos
|
2005
|
0.80
|
|
35
|
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.
|
J Pharm Biomed Anal
|
2007
|
0.80
|
|
36
|
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.
|
J Med Chem
|
2003
|
0.79
|
|
37
|
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.
|
Drug Metab Dispos
|
2009
|
0.79
|
|
38
|
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).
|
Drug Metab Dispos
|
2009
|
0.79
|
|
39
|
In vitro screening of 50 highly prescribed drugs for thiol adduct formation--comparison of potential for drug-induced toxicity and extent of adduct formation.
|
Chem Res Toxicol
|
2009
|
0.79
|
|
40
|
Strategy and its implications of protein bioanalysis utilizing high-resolution mass spectrometric detection of intact protein.
|
Anal Chem
|
2011
|
0.79
|
|
41
|
Biotransformation of carbon-14-labeled muraglitazar in male mice: interspecies difference in metabolic pathways leading to unique metabolites.
|
Drug Metab Dispos
|
2006
|
0.79
|
|
42
|
Plasma stability-dependent circulation of acyl glucuronide metabolites in humans: how circulating metabolite profiles of muraglitazar and peliglitazar can lead to misleading risk assessment.
|
Drug Metab Dispos
|
2010
|
0.78
|
|
43
|
Novel MS solutions inspired by MIST.
|
Bioanalysis
|
2010
|
0.78
|
|
44
|
In vitro assessment of cytochrome P450 inhibition and induction potential of tanespimycin and its major metabolite, 17-amino-17-demethoxygeldanamycin.
|
Cancer Chemother Pharmacol
|
2011
|
0.77
|
|
45
|
Disruption of BSEP Function in HepaRG Cells Alters Bile Acid Disposition and Is a Susceptive Factor to Drug-Induced Cholestatic Injury.
|
Mol Pharm
|
2016
|
0.77
|
|
46
|
Mechanistic studies on a P450-mediated rearrangement of BMS-690514: conversion of a pyrrolotriazine to a hydroxypyridotriazine.
|
Chem Res Toxicol
|
2010
|
0.76
|
|
47
|
Biotransformation profiling of [(14)C]ixabepilone in human plasma, urine and feces samples using accelerator mass spectrometry (AMS).
|
Drug Metab Pharmacokinet
|
2009
|
0.76
|
|
48
|
Metabolism and disposition of [14C]BMS-690514 after oral administration to rats, rabbits, and dogs.
|
Drug Metab Dispos
|
2010
|
0.76
|
|
49
|
In vitro characterization of the metabolic pathways and cytochrome P450 inhibition and induction potential of BMS-690514, an ErbB/vascular endothelial growth factor receptor inhibitor.
|
Drug Metab Dispos
|
2011
|
0.75
|
|
50
|
Integrated quantitative and qualitative workflow for in vivo bioanalytical support in drug discovery using hybrid Q-TOF-MS.
|
Bioanalysis
|
2012
|
0.75
|
|
51
|
Bioactivation of substituted thiophenes including α-chlorothiophene-containing compounds in human liver microsomes.
|
Chem Res Toxicol
|
2011
|
0.75
|
|
52
|
Glucuronidation as a major metabolic clearance pathway of 14c-labeled muraglitazar in humans: metabolic profiles in subjects with or without bile collection.
|
Drug Metab Dispos
|
2005
|
0.75
|
|
53
|
Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
54
|
Bioactivation of 2-(alkylthio)-1,3,4-thiadiazoles and 2-(alkylthio)-1,3-benzothiazoles.
|
Chem Res Toxicol
|
2012
|
0.75
|
|
55
|
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-2,4-dioxo-1,3,7-triazaspiro[4.4]non7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101) and dasatinib.
|
Drug Metab Dispos
|
2008
|
0.75
|
|
56
|
Pharmacokinetics of muraglitazar (BMS-298585), a dual peroxisome proliferator-activated receptors (PPAR) alpha and gamma activator, in mice, rats, dogs, and monkeys.
|
Xenobiotica
|
2006
|
0.75
|
|
57
|
Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys.
|
Drug Metab Dispos
|
2007
|
0.75
|
|
58
|
Metabolism and disposition of 14C-labeled peliglitazar in humans.
|
Drug Metab Dispos
|
2010
|
0.75
|
|
59
|
Correction to "Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development".
|
J Org Chem
|
2015
|
0.75
|
|
60
|
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
|
Drug Metab Dispos
|
2006
|
0.75
|
|
61
|
Bioactivation of coumarin in rat olfactory mucosal microsomes: Detection of protein covalent binding and identification of reactive intermediates through analysis of glutathione adducts.
|
Chem Biol Interact
|
2009
|
0.75
|
|
62
|
Estimation of the extent of in vivo formation of a mutagenic aromatic amine from a potent thyromimetic compound: correlation of in vitro and in vivo findings.
|
Chem Res Toxicol
|
2011
|
0.75
|
|
63
|
Pharmacokinetics and metabolism of endothelin receptor antagonist: contribution of kidneys in the overall in vivo N-demethylation.
|
Arch Pharm Res
|
2003
|
0.75
|
|
64
|
Identification of human liver microsomal proteins adducted by a reactive metabolite using shotgun proteomics.
|
Chem Res Toxicol
|
2014
|
0.75
|