PMID

Data

Article Title

Organization

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

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Genentech

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

Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.

Genentech

Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.

Bristol-Myers Squibb

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

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

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

Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.

The University Of Tokyo

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.

Abbott Laboratories