Detalles de la búsqueda
1.
Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor.
Mol Pharmacol
; 79(6): 910-20, 2011 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-21372172
2.
JNJ-26070109 [(R)4-bromo-N-[1-(2,4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor antagonist with good oral bioavailability.
J Pharmacol Exp Ther
; 338(1): 328-36, 2011 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-21493750
3.
Characterization of a robust enzymatic assay for inhibitors of 2-oxoglutarate-dependent hydroxylases.
J Biomol Screen
; 14(6): 627-35, 2009 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-19498081
4.
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Bioorg Med Chem Lett
; 19(22): 6373-5, 2009 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19811913
5.
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.
Bioorg Med Chem Lett
; 19(22): 6376-8, 2009 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19815410
6.
Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase.
Bioorg Med Chem Lett
; 19(23): 6548-51, 2009 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19854648
7.
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Bioorg Med Chem
; 16(7): 3917-25, 2008 Apr 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-18289861
8.
Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands.
Bioorg Med Chem Lett
; 17(24): 6905-9, 2007 Dec 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-18029172
9.
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
J Med Chem
; 49(21): 6371-90, 2006 Oct 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-17034143
10.
Species-dependent smooth muscle contraction to Neuromedin U and determination of the receptor subtypes mediating contraction using NMU1 receptor knockout mice.
Br J Pharmacol
; 147(8): 886-96, 2006 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-16474416
11.
Neuromedin U stimulates contraction of human long saphenous vein and gastrointestinal smooth muscle in vitro.
Regul Pept
; 136(1-3): 109-16, 2006 Sep 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-16782214
12.
A novel, quantitative bio-assay for cholecystokinin type-1 receptor activity in the anaesthetised rat.
J Pharmacol Toxicol Methods
; 54(1): 36-41, 2006.
Artículo
en Inglés
| MEDLINE | ID: mdl-16246596
13.
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
J Med Chem
; 48(22): 6790-802, 2005 Nov 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-16250638
14.
Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.
J Med Chem
; 48(22): 6803-12, 2005 Nov 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-16250639
15.
TNF alpha reduces tachykinin, PGE2-dependent, relaxation of the cultured mouse trachea by increasing the activity of COX-2.
Br J Pharmacol
; 144(2): 220-30, 2005 Jan.
Artículo
en Inglés
| MEDLINE | ID: mdl-15665861
16.
Pharmacological analysis of CCK2 receptors up-regulated using engineered transcription factors.
Regul Pept
; 129(1-3): 227-32, 2005 Jul 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-15927720
17.
Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.
Br J Pharmacol
; 172(16): 4078-88, 2015 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-25988595
18.
Cell lines for drug discovery: elevating target-protein levels using engineered transcription factors.
J Biomol Screen
; 9(1): 44-51, 2004 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-15006148
19.
An assay to evaluate the long-term effects of inflammatory mediators on murine airway smooth muscle: evidence that TNFalpha up-regulates 5-HT(2A)-mediated contraction.
Br J Pharmacol
; 137(7): 971-82, 2002 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-12429569
20.
Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
ACS Med Chem Lett
; 1(9): 526-9, 2010 Dec 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-24900242