PMID

Data

Article Title

Organization

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

Discovery of biaryls as ROR¿ inverse agonists by using structure-based design.

Biogen

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)

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.

Genentech

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 biaryl carboxylamides as potent ROR¿ inverse agonists.

Biogen Idec

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

A reversed sulfonamide series of selective RORc inverse agonists.

Argenta Discovery

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

Identification of tertiary sulfonamides as RORc inverse agonists.

Genentech

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

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

Recent progress on nuclear receptor ROR? modulators.

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

Discovery of [1,2,4]Triazolo[1,5-

Teijin Pharma

3-Substituted Quinolines as ROR?t Inverse Agonists.

Janssen Research And Development

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists.

Bristol-Myers Squibb

Discovery of N-indanyl benzamides as potent ROR?t inverse agonists.

Fudan University

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

Structure-Based and Property-Driven Optimization of

Global Discovery Chemistry

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

Sulfoximines as potent ROR? inverse agonists.

Nestle Skin Health

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 carbazole carboxamides as novel ROR?t inverse agonists.

Fudan University

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

6-Substituted quinolines as ROR?t inverse agonists.

Janssen Research And Development

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

From ROR?t Agonist to Two Types of ROR?t Inverse Agonists.

Fudan University

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

Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.

Washington University

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

Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.

Friedrich Alexander University Erlangen

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

Novartis

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

Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands.

Purdue University

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

Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.

Sapienza University Of Rome

Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.

Boehringer Mannheim