Detalhe da pesquisa
1.
Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists.
Bioorg Med Chem Lett
; 78: 129021, 2022 12 15.
Artigo
Inglês
| MEDLINE | ID: mdl-36228968
2.
Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists.
Bioorg Med Chem Lett
; 76: 128988, 2022 11 15.
Artigo
Inglês
| MEDLINE | ID: mdl-36113671
3.
Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.
Bioorg Med Chem Lett
; 30(18): 127418, 2020 09 15.
Artigo
Inglês
| MEDLINE | ID: mdl-32750526
4.
Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett
; 29(1): 47-50, 2019 01 01.
Artigo
Inglês
| MEDLINE | ID: mdl-30446311
5.
VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Bioorg Med Chem Lett
; 29(14): 1714-1718, 2019 07 15.
Artigo
Inglês
| MEDLINE | ID: mdl-31113706
6.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-31248774
7.
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.
Bioorg Med Chem Lett
; 29(2): 342-346, 2019 01 15.
Artigo
Inglês
| MEDLINE | ID: mdl-30503632
8.
Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.
Mol Pharmacol
; 93(5): 526-540, 2018 05.
Artigo
Inglês
| MEDLINE | ID: mdl-29545267
9.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-29705142
10.
Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).
Drug Metab Dispos
; 45(12): 1245-1259, 2017 12.
Artigo
Inglês
| MEDLINE | ID: mdl-28939686
11.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-28958625
12.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-26988308
13.
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead.
Bioorg Med Chem Lett
; 24(4): 1067-70, 2014 Feb 15.
Artigo
Inglês
| MEDLINE | ID: mdl-24461352
14.
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bioorg Med Chem Lett
; 24(15): 3307-14, 2014 Aug 01.
Artigo
Inglês
| MEDLINE | ID: mdl-24969015
15.
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
Bioorg Med Chem Lett
; 23(13): 3713-8, 2013 Jul 01.
Artigo
Inglês
| MEDLINE | ID: mdl-23727046
16.
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bioorg Med Chem Lett
; 23(21): 5779-85, 2013 Nov 01.
Artigo
Inglês
| MEDLINE | ID: mdl-24074843
17.
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.
Mol Pharmacol
; 82(5): 860-75, 2012 Nov.
Artigo
Inglês
| MEDLINE | ID: mdl-22863693
18.
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
Drug Metab Dispos
; 40(9): 1834-45, 2012 Sep.
Artigo
Inglês
| MEDLINE | ID: mdl-22711749
19.
Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
Bioorg Med Chem Lett
; 22(1): 76-81, 2012 Jan 01.
Artigo
Inglês
| MEDLINE | ID: mdl-22172704
20.
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.
J Med Chem
; 65(8): 6273-6286, 2022 04 28.
Artigo
Inglês
| MEDLINE | ID: mdl-35417155