Detalhe da pesquisa
1.
Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro.
Bioorg Med Chem Lett
; 74: 128923, 2022 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-35944850
2.
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
em Inglês
| MEDLINE | ID: mdl-36228968
3.
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
em Inglês
| MEDLINE | ID: mdl-36113671
4.
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.
Mol Psychiatry
; 25(11): 2786-2799, 2020 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-30116027
5.
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.
Bioorg Med Chem Lett
; 47: 128193, 2021 09 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-34118412
6.
Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model.
Bioorg Med Chem Lett
; 37: 127838, 2021 04 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-33556572
7.
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
em Inglês
| MEDLINE | ID: mdl-32750526
8.
Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.
Bioorg Med Chem Lett
; 30(22): 127529, 2020 11 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-32890686
9.
Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain.
Proc Natl Acad Sci U S A
; 114(10): E1996-E2005, 2017 03 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-28223516
10.
Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063.
J Pharmacol Exp Ther
; 370(3): 350-359, 2019 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-31201216
11.
Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu3 NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy.
Bioorg Med Chem Lett
; 29(18): 2670-2674, 2019 09 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31358468
12.
Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278.
Bioorg Med Chem Lett
; 29(10): 1211-1214, 2019 05 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30910459
13.
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
em Inglês
| MEDLINE | ID: mdl-30446311
14.
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
em Inglês
| MEDLINE | ID: mdl-30503632
15.
Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.
Mol Pharmacol
; 94(2): 926-937, 2018 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-29895592
16.
Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives.
Bioorg Med Chem Lett
; 28(23-24): 3670-3673, 2018 12 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30528979
17.
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
em Inglês
| MEDLINE | ID: mdl-29705142
18.
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.
Bioorg Med Chem Lett
; 28(12): 2175-2179, 2018 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29754948
19.
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.
Bioorg Med Chem Lett
; 28(15): 2641-2646, 2018 08 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29958762
20.
Contributions of Protease-Activated Receptors PAR1 and PAR4 to Thrombin-Induced GPIIbIIIa Activation in Human Platelets.
Mol Pharmacol
; 91(1): 39-47, 2017 Jan.
Artigo
em Inglês
| MEDLINE | ID: mdl-27784794