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1.
Application of Covalent Binding Body Burden in the HµREL Human Hepatocyte Coculture Model for Reactivity Risk Assessment of Metabolically Low Turnover Drugs.
Chem Res Toxicol;
37(4): 540-544, 2024 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-38530825
2.
Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human.
Drug Metab Dispos;
50(8): 1064-1076, 2022 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-35680134
3.
Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
J Med Chem;
66(4): 2877-2892, 2023 02 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-36757100
4.
A Phase 1 First-in-Human Pharmacokinetic and Pharmacodynamic Study of JNJ-64264681, a Covalent Inhibitor of Bruton's Tyrosine Kinase.
Clin Pharmacol Drug Dev;
12(6): 611-624, 2023 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-37125450
5.
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
J Med Chem;
65(21): 14326-14336, 2022 11 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-36314537
6.
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
ACS Med Chem Lett;
12(5): 782-790, 2021 May 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-34055226
7.
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
ACS Med Chem Lett;
11(10): 2002-2009, 2020 Oct 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-33062185
8.
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
J Med Chem;
63(17): 9181-9196, 2020 09 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32787105
9.
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
ACS Med Chem Lett;
10(3): 261-266, 2019 Mar 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-30891123
10.
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
J Med Chem;
61(1): 207-223, 2018 01 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-29211470
11.
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
J Med Chem;
60(11): 4559-4572, 2017 06 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-28493698
12.
Cytosolic heat shock proteins and heme oxygenase-1 are preferentially induced in response to specific and localized intramitochondrial damage by tetrafluoroethylcysteine.
Biochem Pharmacol;
72(1): 80-90, 2006 Jun 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-16678137
13.
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
J Med Chem;
59(18): 8535-48, 2016 09 22.
Artículo
en Inglés
| MEDLINE | ID: mdl-27548392
14.
The fragmented mitochondrial ribosomal RNAs of Plasmodium falciparum.
PLoS One;
7(6): e38320, 2012.
Artículo
en Inglés
| MEDLINE | ID: mdl-22761677
15.
Comparison of in vitro bioactivation of flutamide and its cyano analogue: evidence for reductive activation by human NADPH:cytochrome P450 reductase.
Chem Res Toxicol;
21(12): 2393-406, 2008 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-19548358
16.
Comparison of the cytotoxicity of the nitroaromatic drug flutamide to its cyano analogue in the hepatocyte cell line TAMH: evidence for complex I inhibition and mitochondrial dysfunction using toxicogenomic screening.
Chem Res Toxicol;
20(9): 1277-90, 2007 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-17702527
17.
Profiling the hepatic effects of flutamide in rats: a microarray comparison with classical aryl hydrocarbon receptor ligands and atypical CYP1A inducers.
Drug Metab Dispos;
34(7): 1266-75, 2006 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-16611858
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