PMID

Data

Article Title

Organization

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

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.

Vitae Pharmaceuticals

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

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

Genentech

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

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

Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.

The University Of Tokyo

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.

Genentech

Identification of New Nonsteroidal ROR? Ligands; Related Structure-Activity Relationships and Docking Studies.

Genfit

The evolution paths of some reprehensive scaffolds of ROR?t modulators, a perspective from medicinal chemistry.

Sun Yat-Sen University

Defining Target Engagement Required for Efficacy

Lilly Research Laboratories

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

Withanolide Derivative 2,3-Dihydro-3?-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor ? (RORa).

National Institute Of Advanced Industrial Science And Technology (Aist)

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 carboxyl-containing biaryl ureas as potent ROR?t inverse agonists.

Fudan University

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

Tricyclic sulfones as potent, selective and efficacious ROR?t inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.

Bristol Myers Squibb

Novel Tricyclic Pyroglutamide Derivatives as Potent ROR?t Inverse Agonists Identified using a Virtual Screening Approach.

Bristol Myers Squibb

Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists.

Bristol Myers Squibb

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

Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.

Advinus Therapeutics

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

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

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

Potent and Orally Bioavailable Inverse Agonists of ROR?t Resulting from Structure-Based Design.

Astrazeneca

Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

TBA