Detalhe da pesquisa
1.
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Cell
; 161(6): 1252-65, 2015 Jun 04.
Artigo
em Inglês
| MEDLINE | ID: mdl-26046436
2.
Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in ß-amino carboxamide-harboring ligands.
Bioorg Med Chem Lett
; 29(3): 362-366, 2019 02 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-30580918
3.
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
em Inglês
| MEDLINE | ID: mdl-31113706
4.
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
em Inglês
| MEDLINE | ID: mdl-31248774
5.
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.
Artigo
em Inglês
| MEDLINE | ID: mdl-26508634
6.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.
Bioorg Med Chem Lett
; 27(13): 2990-2995, 2017 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28522253
7.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Bioorg Med Chem Lett
; 27(23): 5179-5184, 2017 12 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29089231
8.
Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.
Bioorg Med Chem Lett
; 27(2): 171-175, 2017 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27939174
9.
Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.
Bioorg Med Chem Lett
; 27(11): 2296-2301, 2017 06 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28442253
10.
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.
Bioorg Med Chem Lett
; 26(17): 4282-6, 2016 09 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27476142
11.
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Bioorg Med Chem Lett
; 26(13): 3029-3033, 2016 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27185330
12.
M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location.
J Neurosci
; 34(9): 3253-62, 2014 Feb 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-24573284
13.
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.
Bioorg Med Chem Lett
; 25(3): 690-4, 2015 Feb 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-25542588
14.
(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.
Bioorg Med Chem Lett
; 24(1): 258-61, 2014 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-24332093
15.
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Bioorg Med Chem Lett
; 24(19): 4708-4713, 2014 Oct 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-25176330
16.
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.
Bioorg Med Chem Lett
; 23(6): 1860-4, 2013 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23416001
17.
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Bioorg Med Chem Lett
; 23(10): 2996-3000, 2013 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23562060
18.
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.
Bioorg Med Chem Lett
; 23(2): 412-6, 2013 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23237839
19.
Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.
Bioorg Med Chem Lett
; 23(1): 346-50, 2013 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-23177787
20.
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.
Bioorg Med Chem Lett
; 23(1): 223-7, 2013 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-23200253