45 articles for thisTarget
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Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Tsukuba Research Institute
Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.
Tsukuba Research Institute
Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor.
Tsukuba Research Institute
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
Tsukuba Research Institute
Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist.
Tsukuba Research Institute
Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.
Tsukuba Research Institute
Identification of positron emission tomography ligands for NPY Y5 receptors in the brain.
Tsukuba Research Institute
Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.
Tsukuba Research Institute
Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
Tsukuba Research Institute
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors.
Tsukuba Research Institute
Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Tsukuba Research Institute
Novel orally active NPY Y5 receptor antagonists: Synthesis and structure-activity relationship of spiroindoline class compounds.
Tsukuba Research Institute
Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists.
Tsukuba Research Institute
Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists.
Tsukuba Research Institute
Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Tsukuba Research Institute
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.
Tsukuba Research Institute
Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity.
Tsukuba Research Institute
Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R).
Tsukuba Research Institute
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
Tsukuba Research Institute
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.
Tsukuba Research Institute
Aryl urea derivatives of spiropiperidines as NPY Y5 receptor antagonists.
Tsukuba Research Institute
Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
Tsukuba Research Institute
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and biological activities of topoisomerase I inhibitors, 6-arylmethylamino analogues of edotecarin.
Tsukuba Research Institute
Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Tsukuba Research Institute
Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists.
Tsukuba Research Institute
Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.
Tsukuba Research Institute
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Tsukuba Research Institute
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
(9S)-9-(2-hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2,3,4,9-tetrahydro-1H-xanthen-1-one, a selective and orally active neuropeptide Y Y5 receptor antagonist.
Tsukuba Research Institute
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
Tsukuba Research Institute
Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
Tsukuba Research Institute
Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.
Tsukuba Research Institute
Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.
Tsukuba Research Institute
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.
Tsukuba Research Institute
Synthesis and evaluation of substituted 4-alkoxy-2-aminopyridines as novel neuropeptide Y1 receptor antagonists.
Tsukuba Research Institute
Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.
Tsukuba Research Institute
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.
Tsukuba Research Institute
A new class of highly potent farnesyl diphosphate-competitive inhibitors of farnesyltransferase.
Tsukuba Research Institute