256 articles for thisTarget
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Article Title
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Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Instituto De Qu£Mica M£Dica (Iqm-Csic)
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor.
The Scripps Research Institute
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties.
Ochanomizu University
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.
Bristol-Myers Squibb
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.
Vitae Pharmaceuticals
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
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.
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.
Astrazeneca
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
Eli Lilly
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
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.
Seragon Pharmaceuticals
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.
TBA
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.
Boehringer Ingelheim (Canada)
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.
Novartis Institutes For Biomedical Research
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Bristol-Myers Squibb
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.
Boehringer Ingelheim Pharmaceuticals
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Astrazeneca
Identification of the first potent, selective and bioavailable PPARa antagonist.
Inception Sciences
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.
Pfizer
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.
Boehringer Ingelheim Pharmaceuticals
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.
Boehringer Ingelheim Pharmaceuticals
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Eli Lilly
Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands.
Boehringer Ingelheim Pharmaceuticals
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.
Pfizer
Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.
Bristol-Myers Squibb
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Ironwood Pharmaceuticals
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.
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.
Takeda Pharmaceutical
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Glaxosmithkline
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.
Glaxosmithkline
Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents.
Zydus Research Centre
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.
Trinity College
Discovery of a potent series of non-steroidal nona-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Glaxosmithkline
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Merck Research Laboratories
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora.
Charles University In Prague
Discovery of quinolines as selective glucocorticoid receptor agonists.
Bayer Schering Pharma
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
Glaxosmithkline
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
Medicines Research Centre
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Glaxosmithkline
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Glaxosmithkline
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
Glaxosmithkline
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
Glaxosmithkline
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
Schering
Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.
Corcept Therapeutics
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.
Pfizer
Discovery of selective glucocorticoid receptor modulator MK-5932.
Merck Research Laboratories
Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).
Merck Research Laboratories
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.
Bristol-Myers Squibb
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Ursodeoxycholic acid amides as novel glucocorticoid receptor modulators.
Trinity College Dublin
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.
Boehringer Ingelheim Pharmaceuticals
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
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.
Pfizer
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.
Pfizer
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
Pfizer
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy of Sciences
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.
University of Illinois
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.
Trinity College
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.
Wyeth Research
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
Bristol-Myers Squibb
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides.
University of Texas Southwestern Medical Center
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Bristol-Myers Squibb
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Wyeth Research
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Wyeth Research
Sundaicumones A and B, polyprenylated acylphloroglucinol derivatives from Calophyllumsundaicum with weak activity against the glucocorticoid receptor.
Merlion Pharmaceuticals
High-throughput evaluation of relative cell permeability between peptoids and peptides.
University of Texas Southwestern Medical Center
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Ligand Pharmaceuticals
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
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).
Wyeth Research
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Corcept Therapeutics
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
Rti International
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Corcept Therapeutics
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
Johnson & Johnson Pharmaceutical Research & Development
Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.
Boehringer Ingelheim Pharmaceuticals
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Abbott Laboratories
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Abbott Laboratories
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
Boehringer Ingelheim Pharmaceuticals
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
University of Perugia
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
Boehringer Ingelheim Pharmaceuticals
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
The Pennsylvania State University
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Abbott Laboratories
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
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.
Women'S Health Research Institute
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
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.
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.
Ligand Pharmaceuticals
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Ligand Pharmaceuticals
Anti-inflammatory 17beta-thioalkyl-16alpha,17alpha-ketal and -acetal androstanes: a new class of airway selective steroids for the treatment of asthma.
Rh£Ne-Poulenc Rorer Central Research
Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17 alpha-esters containing a functional group.
Mitsubishi Kasei
Dexamethasone 21-(beta-isothiocyanatoethyl) thioether: a new affinity label for glucocorticoid receptors.
Niddk
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.
Wyeth Research
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
Abbott Laboratories
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Ligand Pharmaceuticals
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Ligand Pharmaceuticals
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Ligand Pharmaceuticals
Synthesis and antihormonal properties of novel 11ß-benzoxazole-substituted steroids.
Research Triangle Institute
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).
Merck Research Laboratories
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.
Merck Research Laboratories
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.
Boehringer Ingelheim Pharmaceuticals
Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
Kaken Pharmaceutical
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-791
Bristol-Myers Squibb
6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence.
Ochanomizu University
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
Pfizer
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
Vitae Pharmaceuticals
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.
Ligand Pharmaceuticals
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.
Ligand Pharmaceuticals
Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
Kaken Pharmaceutical
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.
Ligand Pharmaceuticals
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
Monash University (Parkville Campus)
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
Ligand Pharmaceuticals
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Vitae Pharmaceuticals
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Amgen
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.
Pfizer
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
Pfizer
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Glaxosmithkline
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.
Pfizer
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.
Medicines Research Centre
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.
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.
Ligand Pharmaceuticals
Expanding the repertoire of small molecule transcriptional activation domains.
University of Michigan
(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.
Eli Lilly
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
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.
Wyeth Research
Discovery of PPARγ and glucocorticoid receptor dual agonists to promote the adiponectin and leptin biosynthesis in human bone marrow mesenchymal stem cells.
Seoul National University
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.
Argenta Discovery
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.
Griffith University
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.
Ligand Pharmaceuticals
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Guangdong Pharmaceutical University
Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer.
Shanghai Institute of Materia Medica
Identification of 1,2,3-triazolium salt-based inhibitors of Leishmania infantum trypanothione disulfide reductase with enhanced antileishmanial potency in cellulo and increased selectivity.
Universidad De Alcal£
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
University of Innsbruck
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
Schr£Dinger
A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol.
Boehringer Ingelheim Pharmaceuticals
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
Mitsubishi Tanabe Pharma
Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses.
University of Tennessee
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Merck Research Laboratories
Discovery of novel non-steroidal selective glucocorticoid receptor modulators by structure- and IGN-based virtual screening, structural optimization, and biological evaluation.
Zhejiang University
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
F. Hoffmann-La Roche
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Merck Research Laboratories
Discovery of a Novel Androgen Receptor Antagonist Manifesting Evidence to Disrupt the Dimerization of the Ligand-Binding Domain via Attenuating the Hydrogen-Bonding Network Between the Two Monomers.
Zhejiang University
α/Sulfono-γ-AApeptide Hybrid Analogues of Glucagon with Enhanced Stability and Prolonged In Vivo Activity.
University of South Florida
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
University of California San Francisco
The Flavonoid Baicalein Negatively Regulates Progesterone Target Genes in the Uterus
University of Illinois At Chicago
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
Abbott Laboratories
Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion.
University of Tennessee
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Abbott Laboratories
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Janssen Research and Development
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Ligand Pharmaceuticals
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.
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.
Abbott Laboratories
Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD).
Mitobridge
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Merck And
Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1).
Sk Chemicals
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
Deacylcortivazol-like pyrazole regioisomers reveal a more accommodating expanded binding pocket for the glucocorticoid receptor.
University of Iowa
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.
Abbott Laboratories
Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist.
Zhejiang Normal University
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Abbott Laboratories
Novel glucocorticoid antedrugs possessing a 17beta-(gamma-lactone) ring.
Glaxo Wellcome Research and Development
Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
Pharmaron-Beijing
Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.
Glaxo Wellcome Research and Development
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Oric Pharmaceuticals
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
Ligand Pharmaceuticals
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
Ligand Pharmaceuticals
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.
Merck
Profiling withanolide A for therapeutic targets in neurodegenerative diseases.
University of Basel
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Inception Sciences
Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor.
European Institute of Chemistry and Biology (Iecb)
Quantitative and systems pharmacology 4. Network-based analysis of drug pleiotropy on coronary artery disease.
Guangzhou University of Chinese Medicine
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
Eli Lilly
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.
Corcept Therapeutics
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.
Forschungszentrum Dresden-Rossendorf
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).
Marquette University
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Astrazeneca
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
TBA
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Oric Pharmaceuticals
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
The University of Tokyo
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.
Corcept Therapeutics
Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold.
The University of Tokyo
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Astrazeneca
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Pfizer
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Takeda Pharmaceutical
Quinoline-based compounds and methods of inhibiting CDK8/19
University of South Carolina
NOVEL BIARYL DERIVATIVE USEFUL AS DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITOR, AND USE THEREOF
Lg Chem
Method for preparing pyrrolo[3,2-D]pyrimidine compound, and intermediates thereof
Chia Tai Tianqing Pharmaceutical Group
Heterocyclylalkyne derivatives and their use as modulators of mGluR5 receptors
Recordati Ireland
Nicotinamide adenine dinucleotide-induced multimerization of the co-repressor CtBP1 relies on a switching tryptophan.
Oregon Health and Science University
MRSA Isolates from United States Hospitals Carry dfrG and dfrK Resistance Genes and Succumb to Propargyl-Linked Antifolates.
University of Connecticut
Inhibition studies of porphobilinogen synthase from Escherichia coli differentiating between the two recognition sites.
University of NeuchÂTel
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center