rorγ

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.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

Methyl-3β-hydroxycholenate (Methyl 3beta-hydroxychol-5-enoate) is a modulator of RORγ.

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

SR2211 is a specific modulator and an inverse agonist of RORγ(IC50 = 320 nM, Ki = 105 nM).

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.

Zymostenol (5a-Cholest-8-en-3b-ol) is a RORγ agonist with an EC50 of 1 μM and serves as a late-stage precursor in cholesterol biosynthesis.

GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.

SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).

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).

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).

Cintirorgon (LYC-55716) is a selective, oral agonist of RORγ, modulating gene expression in RORγ-expressing T lymphocyte immune cells.

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

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.

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.

RORγinverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC50 values of 0.4 μM for Gal4-RORγ and 0.9 μM for full-length RORγ. This compound is useful for researching autoimmune diseases.

RORγ agonist2 (Compound 34) is a selective RORγ agonist with an EC50 of 0.03 μM for hRORγ. It significantly inhibits tumor growth in an MC38 tumor mouse model with the same genetic background.

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.

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].

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.