PMID

Data

Article Title

Organization

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.

Universit£

Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.

Broad Institute Of Mit And Harvard

Macrolactonolides: a novel class of anti-inflammatory compounds.

Glaxosmithkline

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

Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.

Corcept Therapeutics

Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.

Pfizer

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

5-Functionalized indazoles as glucocorticoid receptor agonists.

Amri

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

Alkaloids from the Australian rainforest tree Ochrosia moorei.

Griffith University

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.

Universit£

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

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

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

Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.

Ligand Pharmaceuticals

Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids

TBA

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

Optimisation of a pyrazole series of progesterone antagonists; Part 1.

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 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

The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.

University Of Innsbruck

A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol.

Boehringer Ingelheim Pharmaceuticals

Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.

Merck Research Laboratories

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

Merck Research Laboratories

Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.

University Of California San Francisco

Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.

Abbott Laboratories

Discovery of novel nonsteroidal glucocorticoid receptor modulators.

Abbott Laboratories

Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

Abbott Laboratories

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

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

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

Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.

Glaxo Wellcome Research And Development

Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.

Ligand Pharmaceuticals

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

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.

Ligand Pharmaceuticals