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1.
NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations.
Cancer Discov
; 13(3): 598-615, 2023 03 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-36511802
2.
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Chem Res Toxicol
; 23(6): 1115-26, 2010 Jun 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-20507089
3.
Evaluation of the metabolism of propranolol by linear ion trap technology in mouse, rat, dog, monkey, and human cryopreserved hepatocytes.
Rapid Commun Mass Spectrom
; 23(14): 2146-50, 2009 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-19517456
4.
High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.
Curr Drug Metab
; 9(9): 847-53, 2008 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-18991580
5.
Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose.
Chem Res Toxicol
; 21(9): 1814-22, 2008 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-18690722
6.
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Bioorg Med Chem Lett
; 18(23): 6071-7, 2008 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-18951788
7.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
J Med Chem
; 49(14): 4425-36, 2006 Jul 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-16821801
8.
Application of a linear ion trap/orbitrap mass spectrometer in metabolite characterization studies: examination of the human liver microsomal metabolism of the non-tricyclic anti-depressant nefazodone using data-dependent accurate mass measurements.
J Am Soc Mass Spectrom
; 17(3): 363-75, 2006 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-16442304
9.
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
ACS Med Chem Lett
; 7(9): 862-7, 2016 Sep 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-27660692
10.
Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4.
Chem Biol Interact
; 155(1-2): 10-20, 2005 Jun 30.
Artículo
en Inglés
| MEDLINE | ID: mdl-15978881
11.
Minimising the potential for metabolic activation in drug discovery.
Expert Opin Drug Metab Toxicol
; 1(1): 91-142, 2005 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-16922655
12.
The development of a higher throughput reactive intermediate screening assay incorporating micro-bore liquid chromatography-micro-electrospray ionization-tandem mass spectrometry and glutathione ethyl ester as an in vitro conjugating agent.
J Pharm Biomed Anal
; 36(1): 105-16, 2004 Sep 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-15351054
13.
NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine.
Chem Res Toxicol
; 20(11): 1649-57, 2007 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-17907785
14.
A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.
Chem Res Toxicol
; 20(12): 1954-65, 2007 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-17935300
15.
A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues.
Chem Res Toxicol
; 19(3): 480-90, 2006 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-16544956
16.
Detection and quantification of N-(deoxyguanosin-8-yl)-4-aminobiphenyl adducts in human pancreas tissue using capillary liquid chromatography-microelectrospray mass spectrometry.
Chem Res Toxicol
; 18(4): 692-9, 2005 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-15833029
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