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156 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.EBI
Bristol-Myers Squibb Research & Development
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.EBI
Vitae Pharmaceuticals
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.EBI
Central Pharmaceutical Research Institute
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
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.EBI
Astrazeneca
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
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.EBI
TBA
Development of 1,3-diphenyladamantane derivatives as nonsteroidal progesterone receptor antagonists.EBI
Tokyo Medical And Dental University
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.EBI
Novartis Institutes For Biomedical Research
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
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
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.EBI
Glaxosmithkline
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.EBI
Trinity College
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.EBI
Merck Research Laboratories
Discovery of quinolines as selective glucocorticoid receptor agonists.EBI
Bayer Schering Pharma
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.EBI
Glaxosmithkline
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.EBI
Medicines Research Centre
2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists.EBI
Glaxosmithkline
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.EBI
Glaxosmithkline
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.EBI
Schering
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.EBI
Pfizer
Discovery of diarylhydantoins as new selective androgen receptor modulators.EBI
Galapagos, Parc Biocitech
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
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.EBI
University Of Illinois
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.EBI
Wyeth Research
Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.EBI
University Of Quebec At Trois-Rivieres
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.EBI
Bristol-Myers Squibb
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.EBI
Johnson And Johnson Pharmaceutical Research And Development
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.EBI
Bristol-Myers Squibb
Syntheses and antigestagenic activity of mifepristone derivatives.EBI
University Of Graz
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
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.EBI
Nv Organon
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.EBI
Rti International
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.EBI
Johnson & Johnson Pharmaceutical Research & Development
Identification of dissociated non-steroidal glucocorticoid receptor agonists.EBI
Boehringer Ingelheim Pharmaceuticals
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.EBI
Johnson And Johnson Pharmaceutical Research And Development
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.EBI
Johnson And Johnson Pharmaceutical Research And Development
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
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.EBI
University Of Ferrara
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.EBI
Abbott Laboratories
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.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
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.EBI
Pfizer
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.EBI
Ligand Pharmaceuticals
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.EBI
Ligand Pharmaceuticals
5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.EBI
Ligand Pharmaceuticals
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.EBI
Ligand Pharmaceuticals
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.EBI
Ligand Pharmaceuticals
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.EBI
Ligand Pharmaceuticals
Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors.EBI
R. W. Johnson Pharmaceutical Research Institute
Novel pyrrole-containing progesterone receptor modulators.EBI
Wyeth Research
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.EBI
Abbott Laboratories
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.EBI
Wyeth Research
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
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.EBI
Wyeth Research
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.EBI
Wyeth-Ayerst Research
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.EBI
Ligand Pharmaceuticals
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.EBI
Ligand Pharmaceuticals
Synthesis and antihormonal properties of novel 11ß-benzoxazole-substituted steroids.EBI
Research Triangle Institute
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).EBI
Merck Research Laboratories
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.EBI
Pfizer
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
6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence.EBI
Ochanomizu University
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
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140EBI
TBA
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine FibroidsEBI
TBA
Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor.EBI
Chinese Academy Of Sciences
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
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.EBI
Pfizer
Optimisation of a pyrazole series of progesterone antagonists; Part 1.EBI
Pfizer
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.EBI
Pfizer
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.EBI
Glaxosmithkline
5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators.EBI
Wyeth Research
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.EBI
Glaxosmithkline
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
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.EBI
Glaxosmithkline
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.EBI
Pfizer
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.EBI
Merck Research Laboratories
Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.EBI
The University Of Tokyo
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
SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists.EBI
Nv Organon
(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
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.EBI
Pfizer
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.EBI
Ligand Pharmaceuticals
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.EBI
Wyeth Research
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
SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.EBI
Wyeth Research
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.EBI
Women'S Health Research Institute
SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.EBI
Wyeth Research
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.EBI
Merck Research Laboratories
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.EBI
Glaxosmithkline
Discovery of novel nonsteroidal glucocorticoid receptor modulators.EBI
Abbott Laboratories
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.EBI
Abbott Laboratories
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.EBI
Ligand Pharmaceuticals
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.EBI
Wyeth Research
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.EBI
Abbott Laboratories
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.EBI
Wyeth Research
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.EBI
Abbott Laboratories
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
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.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
Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines.EBI
R. W. Johnson Pharmaceutical Research Institute
Electrostatic Control of Isoform Selective Inhibitor Binding in Nitric Oxide Synthase.BDB
University Of California Irvine