189 articles for thisTarget
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Synthesis of dihydroimidazole tethered imidazolinethiones and their activity as novel antagonists of the nuclear retinoic acid receptor-related orphan receptors (RORs).
Torrey Pines Institute For Molecular Studies
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 RORγt 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 RORγ Inhibitors.
New York University School of Medicine
Small molecule amides as potent ROR-¿ selective modulators.
The Scripps Research Institute
Discovery of Biaryl Amide Derivatives as Potent, Selective, and Orally Bioavailable RORγt Agonists for Cancer Immunotherapy.
Fudan University
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists.
Fudan University
Optimization of carbazole carboxamide RORγt agonists: Challenges in improving the metabolic stability and maintaining the agonistic activity.
Fudan University
Discovery, Synthesis, and In Vitro Characterization of 2,3 Derivatives of 4,5,6,7-Tetrahydro-Benzothiophene as Potent Modulators of Retinoic Acid Receptor-Related Orphan Receptor γt.
Mcgill University
Modes of action insights from the crystallographic structures of retinoic acid receptor-related orphan receptor-γt (RORγt).
Fudan University
Recent advances in small molecule based cancer immunotherapy.
Southern Medical University
Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses.
Cadila Healthcare
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist.
Guangzhou Medical University
Discovery of Chromane-6-Sulfonamide Derivative as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Jiangsu Carefree Pharmaceutical Co.
Agonist Lock Touched and Untouched Retinoic Acid Receptor-Related Orphan Receptor-γt (RORγt) Inverse Agonists: Classification Based on the Molecular Mechanisms of Action.
Fudan University
Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt.
Technische Universiteit Eindhoven
Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
Eindhoven University of Technology
The evolution paths of some reprehensive scaffolds of RORγt 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 RORγ Agonists with Antitumor Activity.
Shanghai Hengrui Pharmaceutical
Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor γt inverse agonists.
Southeast University
Discovery of Orally Available Retinoic Acid Receptor-Related Orphan Receptor γ-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-γ (RORγ) 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 γt agonists.
Fudan University
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Bristol Myers Squibb
Discovery of tetrahydroquinolines and benzomorpholines as novel potent RORγt agonists.
Fudan University
Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists.
Fudan University
Discovery of 6-Oxo-4-phenyl-hexanoic acid derivatives as RORγt 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 RORγt inverse agonists.
Bristol Myers Squibb
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Covalent Occlusion of the RORγt 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 γt inverse agonists for the treatment of autoimmune diseases.
Fudan University
Tricyclic sulfones as potent, selective and efficacious RORγt 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 RORγt inverse agonists.
Bristol Myers Squibb
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists.
Bristol Myers Squibb
Discovery of a Series of Pyrazinone RORγ 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 (RORγ/RORc) inverse agonists.
Bristol Myers Squibb
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.
Inventiva
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Bristol Myers Squibb
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor RORγt.
Reata Pharmaceuticals
Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Phenex Pharmaceuticals
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Phenex Pharmaceuticals
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Bristol Myers Squibb
Discovery of Second Generation RORγ 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 RORγ 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 RORγt inverse agonists.
Bristol-Myers Squibb
Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists.
Technische Universiteit Eindhoven
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Takeda Pharmaceutical
Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists.
Fudan University
Discovery and pharmacological evaluation of indole derivatives as potent and selective RORγt inverse agonist for multiple autoimmune conditions.
Advinus Therapeutics
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt 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 RORγt-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 RORβ 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 (RORγt) 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 RORβ 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 RORγt inverse agonist.
Takeda Pharmaceutical
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Takeda Pharmaceutical
Discovery of orally efficacious RORγt 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 (RORγ/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 RORγt 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 RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
TBA
Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy.
Fudan University
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Janssen Pharmaceutica
Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
Array Biopharma
Imidazooxazole derivative having antitumor effect, and pharmaceutical composition including same
Korea Institute of Science and Technology
5-hydroxytryptamine receptor 7 modulators and their use as therapeutic agents
Temple University
Quinolone derivatives as fibroblast growth factor receptor inhibitors
Principia Biopharma
Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors
Merck Sharp & Dohme
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
The Institute of Cancer Research: Royal Cancer Hospital
Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase
Bristol-Myers Squibb
Benzothiazol compounds and methods using the same for treating neurodegenerative disorders
1St Biotherapeutics
Substituted pyrazole derivatives as selective CDK12/13 inhibitors
Aurigene Discovery Technologies
Small molecule inhibitors of the MCL-1 oncoprotein and uses thereof
University of Maryland, Baltimore
SALT AND CRYSTAL FORM OF DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATE
Nanjing Chia Tai Tianqing Pharmaceutical
Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof
Sanford Burnham Prebys Medical Discovery Institute
2,4-disubstituted phenylene-1,5-diamine derivatives and applications thereof, and pharmaceutical compositions and pharmaceutically acceptable compositions prepared therefrom
Shanghai Haiyan Pharmaceutical Technology
[1,2,4] triazol [4,3-A] pyridine derivative, preparation method therefor or medical application thereof
Jiangsu Hansoh Pharmaceutical
3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof
National Taiwan University
New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation.
University of Orleans
Heterocyclic compounds and uses thereof in the treatment of sexual disorders
Atir Holding
Design, synthesis, and biological evaluation of 3,4,5-trimethoxyphenyl acrylamides as antinarcotic agents.
Ewha Womans University
Structure of the Acinetobacter baumannii dithiol oxidase DsbA bound to elongation factor EF-Tu reveals a novel protein interaction site.
University of Queensland
Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.
University of Toronto
Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.
California Institute of Technology
Symmetrical aryl linked bis-iminothiazolidinones as new chemical entities for the inhibition of monoamine oxidases: Synthesis, in vitro biological evaluation and molecular modelling analysis.
Quaid-I-Azam University
The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.
Soochow University
Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at kappa-opioid receptors in striatal neurons.
The Scripps Research Institute
Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof
President and Fellows of Harvard College
Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
Biomarin Pharmaceutical
Thienopyrimidinone derivatives as mGluR1 antagonists
Korea Institute of Science and Technology
A Fungal-Selective Cytochrome bc1 Inhibitor Impairs Virulence and Prevents the Evolution of Drug Resistance.
Massachusetts Institute of Technology
Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase
Janssen Pharmaceutica
Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
Boehringer Ingelheim International
Design and synthesis of imidazolidine-2,4-dione derivatives as selective inhibitors by targeting protein tyrosine phosphatase-1B over T-cell protein tyrosine phosphatase.
Tianjin Medical University
Uracil compound or salt thereof having human deoxyuridine triphosphatase inhibitory activity
Taiho Pharmaceutical
Acyclic Immucillin Phosphonates: Second-Generation Inhibitors of Plasmodium falciparum Hypoxanthine- Guanine-Xanthine Phosphoribosyltransferase.
Albert Einstein College of Medicine