Detalhe da pesquisa
1.
Discovery of the imidazole-derived GPR40 agonist AM-3189.
Bioorg Med Chem Lett
; 26(1): 15-20, 2016 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26620255
2.
Pharmacological inhibition of polo like kinase 2 (PLK2) does not cause chromosomal damage or result in the formation of micronuclei.
Toxicol Appl Pharmacol
; 269(1): 1-7, 2013 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23466428
3.
Bioactivation of sitaxentan in liver microsomes, hepatocytes, and expressed human P450s with characterization of the glutathione conjugate by liquid chromatography tandem mass spectrometry.
Chem Res Toxicol
; 26(6): 926-36, 2013 Jun 17.
Artigo
em Inglês
| MEDLINE | ID: mdl-23721565
4.
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Bioorg Med Chem Lett
; 23(4): 996-1000, 2013 Feb 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23312944
5.
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Bioorg Med Chem Lett
; 23(9): 2743-9, 2013 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-23522834
6.
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Drug Metab Dispos
; 40(7): 1429-40, 2012 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-22517972
7.
Discovery of potent and specific CXCR3 antagonists.
Bioorg Med Chem Lett
; 22(1): 357-62, 2012 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-22130135
8.
AMG 837: a potent, orally bioavailable GPR40 agonist.
Bioorg Med Chem Lett
; 22(2): 1267-70, 2012 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-22217876
9.
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bioorg Med Chem Lett
; 21(18): 5521-7, 2011 Sep 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21813278
10.
A novel series of IKKß inhibitors part II: description of a potent and pharmacologically active series of analogs.
Bioorg Med Chem Lett
; 21(1): 423-6, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21074992
11.
A novel series of IKKß inhibitors part I: Initial SAR studies of a HTS hit.
Bioorg Med Chem Lett
; 21(1): 417-22, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21074993
12.
Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction.
Drug Metab Dispos
; 38(5): 841-50, 2010 May.
Artigo
em Inglês
| MEDLINE | ID: mdl-20100816
13.
DNL104, a Centrally Penetrant RIPK1 Inhibitor, Inhibits RIP1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers.
Clin Pharmacol Ther
; 107(2): 406-414, 2020 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-31437302
14.
An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
Drug Metab Dispos
; 37(3): 502-13, 2009 Mar.
Artigo
em Inglês
| MEDLINE | ID: mdl-19088267
15.
The conduct of in vitro studies to address time-dependent inhibition of drug-metabolizing enzymes: a perspective of the pharmaceutical research and manufacturers of America.
Drug Metab Dispos
; 37(7): 1355-70, 2009 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-19359406
16.
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
Bioorg Med Chem Lett
; 19(17): 5114-8, 2009 Sep 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19632842
17.
Discovery and optimization of CRTH2 and DP dual antagonists.
Bioorg Med Chem Lett
; 19(22): 6419-23, 2009 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19804971
18.
Tetrahydroquinoline derivatives as CRTH2 antagonists.
Bioorg Med Chem Lett
; 19(24): 6840-4, 2009 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19896843
19.
Imidazo-pyrazine derivatives as potent CXCR3 antagonists.
Bioorg Med Chem Lett
; 19(17): 5200-4, 2009 Sep 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19631529
20.
Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
Bioorg Med Chem Lett
; 18(2): 608-13, 2008 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18063364