175 articles for thisTarget
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Article Title
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Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists.
Galderma R & D
Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new ROR¿ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation.
Jilin University
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
The University of Tokyo
RORc Modulators for the Treatment of Autoimmune Diseases.
Therachem Research Medilab (India)
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR¿t Inhibitors.
Fudan University
Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR¿t inverse agonists.
Fudan University
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists.
Biogen
Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure.
The University of Tokyo
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
Genentech
Discovery of 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide analogs as new RORC modulators.
Boehringer Ingelheim Pharmaceuticals
ROR¿t Modulators Are Potentially Useful for the Treatment of the Immune-Mediated Inflammatory Diseases.
Therachem Research Medilab (India)
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Genentech
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).
Genentech
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
The University of Tokyo
Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new ROR¿ inhibitors using virtual screening, synthesis and biological evaluation.
Chinese Academy of Sciences
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.
The University of Tokyo
Discovery of Tertiary Amine and Indole Derivatives as Potent ROR?t Inverse Agonists.
Glaxosmithkline
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR¿t inhibitors.
Glaxosmithkline
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Genentech
Identification of Potent and Selective Diphenylpropanamide ROR? Inhibitors.
New York University School of Medicine
Small molecule amides as potent ROR-¿ selective modulators.
The Scripps Research Institute
Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor ?t.
Technische Universiteit Eindhoven
Indazole MRL-871 interacts with PPAR? via a binding mode that induces partial agonism.
Eindhoven University of Technology
The evolution paths of some reprehensive scaffolds of ROR?t modulators, a perspective from medicinal chemistry.
Sun Yat-Sen University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Discovery of 2-(Ortho-Substituted Benzyl)-Indole Derivatives as Potent and Orally Bioavailable ROR? Agonists with Antitumor Activity.
Shanghai Hengrui Pharmaceutical
Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor ?t inverse agonists.
Southeast University
Discovery of Orally Available Retinoic Acid Receptor-Related Orphan Receptor ?-t/Dihydroorotate Dehydrogenase Dual Inhibitors for the Treatment of Refractory Inflammatory Bowel Disease.
Fudan University
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-? (ROR?) Agonist for Use in Treating Cancer.
Lycera
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Discovery of novel N-sulfonamide-tetrahydroisoquinolines as potent retinoic acid receptor-related orphan receptor ?t agonists.
Fudan University
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Tricyclic-Carbocyclic ROR?t Inverse Agonists-Discovery of BMS-986313.
Bristol Myers Squibb
Discovery of tetrahydroquinolines and benzomorpholines as novel potent ROR?t agonists.
Fudan University
Discovery of carboxyl-containing biaryl ureas as potent ROR?t inverse agonists.
Fudan University
Discovery of 6-Oxo-4-phenyl-hexanoic acid derivatives as ROR?t inverse agonists showing favorable ADME profile.
Teijin Pharma
Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.
Therapeutics
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel ROR?t inverse agonists.
Bristol Myers Squibb
Azatricyclic Inverse Agonists of ROR?t That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Covalent Occlusion of the ROR?t Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site.
Technische Universiteit Eindhoven
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor ?t inverse agonists for the treatment of autoimmune diseases.
Fudan University
Tricyclic sulfones as potent, selective and efficacious ROR?t inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Bristol Myers Squibb
Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable ROR?t inverse agonists.
Bristol Myers Squibb
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-?t (ROR?t) agonists.
Bristol Myers Squibb
Discovery of a Series of Pyrazinone ROR? Antagonists and Identification of the Clinical Candidate BI 730357.
Boehringer Ingelheim Pharmaceuticals
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (ROR?/RORc) inverse agonists.
Bristol Myers Squibb
Novel Tricyclic Pyroglutamide Derivatives as Potent ROR?t Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active ROR? inverse agonists.
Inventiva
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists.
Bristol Myers Squibb
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR?t.
Reata Pharmaceuticals
Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach.
Phenex Pharmaceuticals
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t.
Phenex Pharmaceuticals
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.
Bristol Myers Squibb
Discovery of Second Generation ROR? Inhibitors Composed of an Azole Scaffold.
Kyoto Prefectural University of Medicine
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.
Genentech
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR? Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.
Bristol-Myers Squibb
Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Inverse Agonists.
Technische Universiteit Eindhoven
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor ?t (ROR?t) Agonist Structure-Based Functionality Switching Approach from In House ROR?t Inverse Agonist to ROR?t Agonist.
Takeda Pharmaceutical
Discovery of aryl-substituted indole and indoline derivatives as ROR?t agonists.
Fudan University
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.
Advinus Therapeutics
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists.
Bristol-Myers Squibb
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR??t Allosteric Inhibitors for Autoimmune Diseases
Merck
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Identification of potent ROR? modulators: Scaffold variation.
The Scripps Research Institute
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Karo Pharma
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (ROR?t) inhibitor, S18-000003.
Shionogi
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
The University of Tokyo
Identification of an aminothiazole series of ROR? modulators.
The Scripps Research Institute
Targeting RORs nuclear receptors by novel synthetic steroidal inverse agonists for autoimmune disorders.
University of Padova
Identification of novel quinazolinedione derivatives as ROR?t inverse agonist.
Takeda Pharmaceutical
Discovery of orally efficacious ROR?t inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Takeda Pharmaceutical
Discovery of orally efficacious ROR?t inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.
Takeda Pharmaceutical
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Identification of fused pyrimidines as interleukin 17 secretion inhibitors.
Norwegian University of Science and Technology
Potent and Orally Bioavailable Inverse Agonists of ROR?t Resulting from Structure-Based Design.
Astrazeneca
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
The University of Tokyo
Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
TBA
Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy.
Fudan University
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Identification and structure activity relationships of quinoline tertiary alcohol modulators of ROR?t.
Janssen Pharmaceutica
Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties.
Universidad De Sevilla
Characterization of the binding of a morphine (mu) receptor-specific ligand: Tyr-Pro-NMePhe-D-Pro-NH2, [3H]-PL17.
Burroughs Wellcome
Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors.
Eli Lilly
Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.
University of Virginia
Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase.
University of California San Francisco
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors.
Dupont Pharmaceuticals
Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors.
Kyoto Prefectural University
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.
Vernalis (R&D)
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
Yale University
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Johnson & Johnson Pharmaceutical
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Inotek Pharmaceuticals
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Vrije Universiteit Amsterdam
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Abbott Laboratories
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.
University of Central Florida College of Medicine
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
Berlex Biosciences
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease.
University of Queensland
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.
Gilead Sciences
Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.
Gilead Sciences
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
Wyeth-Ayerst Research