ROR

RORγ antagonist; inhibits AR expression

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.

TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM.

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases.

Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist.

Cedirogant (ABBV-157) is an orally active RORγt inverse agonist.

S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays.

RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.

Zilovertamab is a humanized monoclonal antibody that inhibits the tumor promoting activity of the cancer stem cell antigen ROR1.

JNJ-61803534 is an effective and orally active RORγt inverse agonist with an IC50 of 9.6 nM. It has anti-inflammatory activity and inhibits the production of IL-17A in human CD4+ T cells under Th17 differentiation conditions.

MRL-871 (compound 3) is an effective inverse agonist of retinoic acid receptor-related orphan receptor gamma t (RORγt), with an IC50 of 264 nM. MRL-871 has a unique imidazole chemical structure and can effectively reduce the generation of IL-17a mRNA in EL4 cells.

RORγt agonist 2 is an effective RORγt activator. It promotes Th17 cell differentiation, increases pro-inflammatory cytokine levels, and enhances lymphocyte cytotoxicity. RORγt agonist 2 inhibits the production of regulatory T cells, thereby suppressing immune responses (extracted from patent WO2021136326A1, compound 23).

ASN06917370 is a former orphan receptor GPR17 ligand for the study of neurodegenerative diseases.

ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor.

W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM.

Desethyl-SID 7969543 is an isoquinolinone analog of SID 7969543 and a selective SF-1 ( NR5A1 ) inhibitor.

Nobiletin is a polymethoxylated flavone extracted from citrus plants. Nobiletin has a variety of pharmacological effects, including antioxidant, anti-inflammatory, and anti-tumor properties.