Detalles de la búsqueda
1.
A fragment-based approach to discovery of Receptor for Advanced Glycation End products inhibitors.
Proteins
; 89(11): 1399-1412, 2021 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-34156100
2.
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
3.
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
4.
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
5.
Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.
Drug Metab Dispos
; 41(9): 1703-14, 2013 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-23821185
6.
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
Bioorg Med Chem Lett
; 22(10): 3467-72, 2012 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22507963
7.
Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3).
J Med Chem
; 64(19): 14757-14772, 2021 10 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-34597046
8.
Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.
J Med Chem
; 63(2): 656-675, 2020 01 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-31858797
9.
Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep
; 26(11): 2916-2928.e13, 2019 03 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-30865883
10.
Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.
J Med Chem
; 61(13): 5623-5642, 2018 07 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-29889518
11.
Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).
ACS Chem Neurosci
; 7(9): 1192-200, 2016 09 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-27075300
12.
High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction.
J Med Chem
; 57(4): 1543-56, 2014 Feb 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-24472025
13.
Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels.
PLoS One
; 8(5): e64905, 2013.
Artículo
en Inglés
| MEDLINE | ID: mdl-23734226
14.
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
Biol Psychiatry
; 73(6): 501-9, 2013 Mar 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23140665
15.
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).
J Med Chem
; 56(20): 7976-96, 2013 Oct 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-24050755
16.
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.
J Med Chem
; 54(21): 7639-47, 2011 Nov 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-21966889
Resultados
1 -
16
de 16
1
Próxima >
>>