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88 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.EBI
Vitae Pharmaceuticals
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.EBI
Eli Lilly
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.EBI
Eli Lilly
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.EBI
TBA
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.EBI
Seragon Pharmaceuticals
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.EBI
Merck Research Laboratories
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.EBI
Bristol-Myers Squibb
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.EBI
Boehringer Ingelheim Pharmaceuticals
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.EBI
Phenex Pharmaceuticals
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.EBI
Takeda Pharmaceutical
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.EBI
Astrazeneca
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.EBI
Pfizer
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.EBI
Merck Research Laboratories
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.EBI
Boehringer Ingelheim Pharmaceuticals
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.EBI
Boehringer Ingelheim Pharmaceuticals
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.EBI
Eli Lilly
Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands.EBI
Boehringer Ingelheim Pharmaceuticals
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.EBI
Boehringer Ingelheim Pharmaceuticals
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.EBI
Pfizer
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists.EBI
University Of Alberta
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.EBI
Ironwood Pharmaceuticals
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.EBI
Bristol-Myers Squibb
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.EBI
Takeda Pharmaceutical
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.EBI
Merck Research Laboratories
Microwave-assisted synthesis of pyrimido[4,5-b][1,6]naphthyridin-4(3H)-ones with potential antitumor activity.EBI
Universidad Del Valle
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.EBI
Merck Research Laboratories
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora.EBI
Charles University In Prague
Discovery of quinolines as selective glucocorticoid receptor agonists.EBI
Bayer Schering Pharma
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.EBI
Medicines Research Centre
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.EBI
Glaxosmithkline
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.EBI
Pfizer
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.EBI
Pfizer
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.EBI
Bristol-Myers Squibb
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.EBI
Boehringer Ingelheim Pharmaceuticals
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.EBI
Pfizer
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.EBI
Pfizer
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.EBI
Pfizer
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.EBI
Chinese Academy Of Sciences
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.EBI
Wyeth Research
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.EBI
Wyeth Research
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.EBI
Wyeth Research
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.EBI
Ligand Pharmaceuticals
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.EBI
Ligand Pharmaceuticals
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).EBI
Wyeth Research
Identification of dissociated non-steroidal glucocorticoid receptor agonists.EBI
Boehringer Ingelheim Pharmaceuticals
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.EBI
Boehringer Ingelheim Pharmaceuticals
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.EBI
Boehringer Ingelheim Pharmaceuticals
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.EBI
Universit£
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.EBI
Boehringer Ingelheim Pharmaceuticals
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.EBI
Abbott Laboratories
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.EBI
Women'S Health Research Institute
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.EBI
Ligand Pharmaceuticals
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.EBI
Abbott Laboratories
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.EBI
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.EBI
Ligand Pharmaceuticals
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.EBI
Ligand Pharmaceuticals
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.EBI
Takeda Pharmaceutical
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.EBI
Boehringer Ingelheim Pharmaceuticals
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791EBI
Bristol-Myers Squibb
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.EBI
Vitae Pharmaceuticals
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.EBI
Ligand Pharmaceuticals
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.EBI
Ligand Pharmaceuticals
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.EBI
Ligand Pharmaceuticals
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine FibroidsEBI
TBA
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.EBI
Ligand Pharmaceuticals
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.EBI
Phenex Pharmaceuticals
Optimisation of a pyrazole series of progesterone antagonists; Part 1.EBI
Pfizer
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.EBI
Pfizer
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.EBI
Glaxosmithkline
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).EBI
Merck Research Laboratories
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.EBI
Ligand Pharmaceuticals
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.EBI
Eli Lilly
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.EBI
Argenta Discovery
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.EBI
Ligand Pharmaceuticals
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.EBI
University Of Innsbruck
Discovery of novel nonsteroidal glucocorticoid receptor modulators.EBI
Abbott Laboratories
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.EBI
Ligand Pharmaceuticals
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.EBI
Abbott Laboratories
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.EBI
Ligand Pharmaceuticals
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.EBI
Ligand Pharmaceuticals
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.EBI
Ligand Pharmaceuticals
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.EBI
Ligand Pharmaceuticals
New steroidal diazo ketones as potential photoaffinity labeling reagents for the mineralocorticoid receptor: synthesis and biological activities.EBI
Université
Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands.BDB
Sun Yat-Sen University