rorγ

Vimirogant is a RORγ inhibitor (Ki: <100 nM).

RORγ-IN-2 (Compound 22) is an inhibitor of RORγ, with a Ki value of 16.6 nM for hRORγ. It is useful for research in IL-17-dependent autoimmune diseases.

XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

RORγ antagonist 1 (compound 22), a potent derivative of betulinic acid, acts as an antagonist to RORγ with a dissociation constant (K D) of 0.18 μM. It demonstrates anti-proliferative effects in the HPAF-II pancreatic cancer xenograft model, inhibits the RAS MAPK and AKT mTORC1 signaling pathways, and triggers caspase-dependent apoptosis in pancreatic cancer cells [1].

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

RORγ agonist 1 is a highly potent and orally bioavailable compound that activates the RORγ receptor. Its efficacy is demonstrated by an EC50 value of 21 nM and it exhibits antitumor activity.

RORγt inverse agonist 32 (compound b14) exhibits oral activity and can be utilized in inflammatory research studies.

RORγt inverse agonist 34 (compound 5a) is an inverse agonist for RORγt, exhibiting an IC50 of 0.094 μM for the inhibition of RORγt-LBD. This compound is utilized in psoriasis research.

RORγt inverse agonist 33 (compound (R)-D4) is an orally bioavailable RORγt inverse agonist with an IC50 of 21 nM, playing a significant role in rheumatoid arthritis research.

RORγt inhibitor 4 (Compound 9a) is an orally active RORγt inhibitor capable of penetrating the central nervous system. It has been shown to improve experimental autoimmune encephalomyelitis.

RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, demonstrating anti-inflammatory activity. It is utilized in the research of rheumatoid arthritis and psoriasis [1].

RORγt inverse agonist 31 (14g) is a potent antagonist of the retinoic acid receptor-related orphan receptor γt (RORγt), with an inhibitory concentration (IC50) of 0.428 μM. It has shown efficacy in reducing Imiquimod-induced psoriasis severity in murine models [1].

RORγt Inverse Agonist 3 is a potent, selective, and orally active inverse agonist of RORγ with EC50 values of 0.22 μM for hRORγ and 0.15 μM for RORγt (human IL-17 cells), respectively.

RORγt modulator 5, a potent RORγt modulator, exhibits a dissociation constant (K_i) of <100 nM. This compound holds promise for the treatment of diseases mediated by RORγ, including inflammatory, metabolic, and autoimmune disorders.

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active, and selective inverse agonist for RORγt with an IC50 of 63.8 nM, exhibiting improved drug-like properties[1].

RORγt agonist 1 is a potent, orally bioavailable agonist of RORγt(EC50 of 20.8 nM).

RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.

RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt, with an EC50 of 119 nM.

RORγt inhibitor 1 is an RORγt allosteric inhibitor with an IC50 value of 1 nM.

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

RORγt Inverse agonist 10 is a highly potent, orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits RORγt activity, a key transcription factor regulating genes linked to psoriasis pathogenesis, including [IL-17A], [IL-22], and [IL-23R].

RORγt DHODH-IN-2 (compound 1) is a potent dual inhibitor of RORγt and DHODH, useful for studying inflammatory bowel disease (IBD).