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44 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Cmpds
Data
Article Title
Organization
39
Ion channels as therapeutic targets: a drug discovery perspective.EBI
Pfizer
19
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.EBI
Merck Sharp Laboratory
149
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.EBI
University of Wisconsin-Milwaukee
14
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.EBI
Merck
4
Triazoloquinazolinediones as novel high affinity ligands for the benzodiazepine site of GABA(A) receptors.EBI
Lund University
7
Developing dual functional allosteric modulators of GABA(A) receptors.EBI
AstraZeneca
3
The GABA(A) receptor as a target for photochromic molecules.EBI
University of Massachusetts
47
Design, synthesis, and subtype selectivity of 3,6-disubstitutedß-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.EBI
University of Wisconsin-Milwaukee
44
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.EBI
F. Hoffmann-La Roche
15
Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.EBI
F. Hoffmann-La Roche
37
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.EBI
Merck Sharp and Dohme Research Laboratories
14
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp & Dohme Research Laboratories
12
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.EBI
TBA
20
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.EBI
Merck Sharp and Dohme Research Laboratories
3
8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.EBI
Merck Sharp and Dohme Research Laboratories
15
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp and Dohme Research Laboratories
9
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp and Dohme Research Laboratories
10
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.EBI
Merck Sharp and Dohme Research Laboratories
31
A new pyridazine series of GABAA alpha5 ligands.EBI
Merck Sharp & Dohme Research Laboratories
1
Pyrazolopyridinones as functionally selective GABAA ligands.EBI
Merck Sharp & Dohme Research Laboratories
100
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.EBI
Merck Sharp & Dohme Research Laboratories
4
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.EBI
Merck Sharp & Dohme Research Laboratories
36
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.EBI
Merck Sharp and Dohme Research Laboratories
1
Neuroactive Type-A γ-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk, EBI
University of Utah
15
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.EBI
Merck Sharp & Dohme Research Laboratories
12
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.EBI
Merck Sharp and Dohme Research Laboratories
62
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.EBI
Merck Sharp and Dohme Research Laboratories
19
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.EBI
The Neuroscience Research Centre
2
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.EBI
University of Wisconsin-Milwaukee
31
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.EBI
Merck Sharp & Dohme Research Laboratories
28
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.EBI
Merck Sharp & Dohme Research Laboratories
12
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.EBI
Merck Sharp & Dohme Research Laboratories
11
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.EBI
The Royal Danish School of Pharmacy
16
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.EBI
Merck Sharp & Dohme Research Laboratories
32
Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABAEBI
University of Sussex
2
Design and Identification of a Novel, Functionally Subtype Selective GABAEBI
Pfizer
58
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.EBI
University of Wisconsin-Milwaukee
7
GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators.EBI
The University of Sydney
32
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptorsEBI
University of Wisconsin-Milwaukee
18
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.EBI
Amgen
60
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.EBI
Roche Pharma Research and Early Development
9
Synthesis and Characterization of a Novelγ-Aminobutyric Acid Type A (GABAEBI
University of Wisconsin-Milwaukee
39
1H-PYRAZOLE-3-AMINE DERIVATIVE HAVING BICYCLIC BACKBONEBDB
Sumitomo Pharma