Detalles de la búsqueda
1.
The effect of the EP3 antagonist DG-041 on male mice with diet-induced obesity.
Prostaglandins Other Lipid Mediat;
144: 106353, 2019 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-31276827
2.
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.
Bioorg Med Chem Lett;
29(16): 2224-2228, 2019 08 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-31248774
3.
mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome.
Hum Mol Genet;
25(10): 1990-2004, 2016 05 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26936821
4.
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett;
28(10): 1679-1685, 2018 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29705142
5.
A novel in vitro allometric scaling methodology for aldehyde oxidase substrates to enable selection of appropriate species for traditional allometry.
Xenobiotica;
48(3): 219-231, 2018 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-28281401
6.
Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice.
Proc Natl Acad Sci U S A;
112(45): 14078-83, 2015 Nov 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-26508634
7.
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett;
27(21): 4858-4866, 2017 11 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28958625
8.
VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.
J Pharmacol Exp Ther;
356(1): 123-36, 2016 Jan.
Artículo
en Inglés
| MEDLINE | ID: mdl-26503377
9.
Evaluating the Disposition of a Mixed Aldehyde Oxidase/Cytochrome P450 Substrate in Rats with Attenuated P450 Activity.
Drug Metab Dispos;
44(8): 1296-303, 2016 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-26936972
10.
Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).
Bioorg Med Chem Lett;
26(13): 2984-2987, 2016 07 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27234146
11.
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.
Bioorg Med Chem Lett;
26(8): 1894-900, 2016 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26988308
12.
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.
Bioorg Med Chem Lett;
26(12): 2915-2919, 2016 06 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27131990
13.
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Bioorg Med Chem Lett;
26(2): 429-434, 2016 Jan 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26684851
14.
VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.
J Infect Dis;
212(9): 1439-48, 2015 Nov 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25883390
15.
Phospholipase D facilitates efficient entry of influenza virus, allowing escape from innate immune inhibition.
J Biol Chem;
289(37): 25405-17, 2014 Sep 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-25065577
16.
A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.
Drug Metab Dispos;
43(11): 1718-26, 2015 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-26265743
17.
Optimization of a small molecule probe that restores e-cadherin expression.
Bioorg Med Chem Lett;
25(19): 4260-4, 2015 Oct 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26299347
18.
Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.
Bioorg Med Chem Lett;
25(13): 2720-5, 2015 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25987377
19.
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.
Bioorg Med Chem Lett;
25(3): 690-4, 2015 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25542588
20.
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Bioorg Med Chem Lett;
25(17): 3515-9, 2015 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26183084