Target family: 1F. Retinoic acid-related orphans (type: nhr)
Target: RAR-related orphan receptor-&gamma;

Ligand: 25-hydroxycholesterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Structural basis for hydroxycholesterols as natural ligands of orphan nuclear receptor RORgamma.
Published in: Mol Endocrinol

Ligand: ALRT 1550 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: AZD0284 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.389999866485596 pIC50
Reference (Journal): AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2
Published in: Journal of Medicinal Chemistry

Ligand: cintirorgon (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Patent): Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease

Ligand: cintirorgon (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Patent): Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease

Ligand: compound 14 [Schnute et al., 2023] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.029999732971191 pIC50
Reference (Journal): Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists
Published in: ACS Medicinal Chemistry Letters

Ligand: compound 25 [Zhang et al., 2020] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Discovery of <i>N</i>-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Published in: ACS Med Chem Lett

Ligand: compound 32 [PMID: 31638797] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pEC50
Reference (Journal): Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Published in: J Med Chem

Ligand: compound 32 [PMID: 31638797] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 10.4399995803833 pIC50
Reference (Patent): Tricyclic sulfones as rorϒ modulators

Ligand: GNE-3500 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.920000076293945 pEC50
Reference (Journal): Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Published in: J Med Chem

Ligand: GSK2981278 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.489999771118164 pIC50
Reference (Journal): Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.
Published in: PLoS ONE

Ligand: MRL-871 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pEC50
Reference (Journal): Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Published in: Bioorg Med Chem Lett

Ligand: RORC2 inverse agonist 66 [PMID: 30130103] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 pIC50
Reference (Journal): 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.
Published in: J Med Chem

Ligand: RORC2 inverse agonist 66 [PMID: 30130103] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.78000020980835 pIC50
Reference (Patent): Methyl-and trifluoromethyl-substituted pyrrolopyridine modulators of rorc2 and methods of use thereof

Ligand: SR1001 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.949999809265137 pKi
Reference (Journal): Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.
Published in: Nature

Ligand: SR1555 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6 pIC50
Reference (Journal): Identification of a selective RORγ ligand that suppresses T(H)17 cells and stimulates T regulatory cells.
Published in: ACS Chem Biol

Ligand: SR2211 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.980000019073486 pKi
Reference (Journal): Identification of SR2211: a potent synthetic RORγ-selective modulator.
Published in: ACS Chem Biol

Ligand: T0901317 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.289999961853027 pKi
Reference (Journal): The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist.
Published in: Mol Pharmacol

Ligand: TAK-828F (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.720000267028809 pIC50
Reference (Journal): Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Published in: J Med Chem

Ligand: XY101 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Published in: J Med Chem

Ligand: XY101 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.119999885559082 pKd
Reference (Journal): Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Published in: J Med Chem

Ligand: XY101 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.420000076293945 pKd
Reference (Journal): Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Published in: J Med Chem