Detalhe da pesquisa
1.
Breakthroughs in neuroactive steroid drug discovery.
Bioorg Med Chem Lett
; 28(2): 61-70, 2018 01 15.
Artigo
Inglês
| MEDLINE | ID: mdl-29223589
2.
Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr-/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator.
J Neurosci Res
; 94(6): 568-78, 2016 Jun.
Artigo
Inglês
| MEDLINE | ID: mdl-26308557
3.
VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease.
J Pharmacol Exp Ther
; 353(2): 405-14, 2015 May.
Artigo
Inglês
| MEDLINE | ID: mdl-25762693
4.
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Nat Chem Biol
; 8(10): 839-47, 2012 Oct.
Artigo
Inglês
| MEDLINE | ID: mdl-22922757
5.
SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
J Med Chem
; 65(13): 9063-9075, 2022 07 14.
Artigo
Inglês
| MEDLINE | ID: mdl-35785990
6.
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.
Bioorg Med Chem Lett
; 20(1): 153-6, 2010 Jan 01.
Artigo
Inglês
| MEDLINE | ID: mdl-19945871
7.
Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.
ACS Med Chem Lett
; 11(10): 1810-1819, 2020 Oct 08.
Artigo
Inglês
| MEDLINE | ID: mdl-33062158
8.
Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator.
Neuropharmacology
; 181: 108333, 2020 12 15.
Artigo
Inglês
| MEDLINE | ID: mdl-32976892
9.
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Bioorg Med Chem Lett
; 19(23): 6529-33, 2009 Dec 01.
Artigo
Inglês
| MEDLINE | ID: mdl-19857967
10.
Neuroactive Steroid N-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.
J Med Chem
; 62(16): 7526-7542, 2019 08 22.
Artigo
Inglês
| MEDLINE | ID: mdl-31390523
11.
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Bioorg Med Chem Lett
; 18(23): 6231-5, 2008 Dec 01.
Artigo
Inglês
| MEDLINE | ID: mdl-18938080
12.
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
ACS Med Chem Lett
; 9(4): 300-305, 2018 Apr 12.
Artigo
Inglês
| MEDLINE | ID: mdl-29670690
13.
Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models.
Epilepsy Res
; 134: 16-25, 2017 08.
Artigo
Inglês
| MEDLINE | ID: mdl-28521115
14.
Neuroactive Steroids. 2. 3α-Hydroxy-3ß-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5ß-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.
J Med Chem
; 60(18): 7810-7819, 2017 09 28.
Artigo
Inglês
| MEDLINE | ID: mdl-28753313
15.
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.
Cancer Discov
; 7(5): 478-493, 2017 05.
Artigo
Inglês
| MEDLINE | ID: mdl-28193778
16.
Allopregnanolone preclinical acute pharmacokinetic and pharmacodynamic studies to predict tolerability and efficacy for Alzheimer's disease.
PLoS One
; 10(6): e0128313, 2015.
Artigo
Inglês
| MEDLINE | ID: mdl-26039057
17.
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.
J Med Chem
; 58(8): 3500-11, 2015 Apr 23.
Artigo
Inglês
| MEDLINE | ID: mdl-25799373
18.
Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.
J Med Chem
; 58(18): 7195-216, 2015 Sep 24.
Artigo
Inglês
| MEDLINE | ID: mdl-26230873
19.
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
J Med Chem
; 57(15): 6668-78, 2014 Aug 14.
Artigo
Inglês
| MEDLINE | ID: mdl-25019388
20.
Dual p38/JNK mitogen activated protein kinase inhibitors prevent ozone-induced airway hyperreactivity in guinea pigs.
PLoS One
; 8(9): e75351, 2013.
Artigo
Inglês
| MEDLINE | ID: mdl-24058677