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

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].

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

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

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

Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).

Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

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).

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].

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

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

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

Bevurogant is an antagonist of RORγt receptor and can be used in studies about the treatment of chronic inflammatory diseases.

Cedirogant (ABBV-157) is an orally active, retinoid-related orphan receptor-γt (RORγt) inverse agonist used in psoriasis studies.

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.

SR0987 is a RORγt agonist,

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding

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

1. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.

SR3335 (ML 176) is a selective inverse agonist of RORα that competitively inhibits the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).

TMP920 inhibits RORγt binding to the SRC1 peptide (IC50: 0.03 μM). TMP920 is a highly potent and selective RORγt antagonist.

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 1.9 nM and a reporter gene IC50 of 6.1 nM.

FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. FM26 is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM.

TMP-778 is a selective inverse agonist of RORγt.

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.

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.

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).

ROR Modulator I is the first potent inverse agonist of the retinoid-related orphan receptor. It also has dual selectivity for RORβ and RORγt.

ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), demonstrating inhibition of IL-17A production from human primary TH17 cells with a pIC50 of 7.5.

RORγt agonist 4 (compound 14) acts as a potent and selective agonist for RORγt, significantly boosting metabolic stability. It also enhances the condition in mouse tumor models, specifically B16F10 melanoma and LLC lung adenocarcinoma [1].

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with an IC50 of 46 nM, making it effective in the treatment of autoimmune diseases by targeting the nuclear receptor RORγt.

RORγt DHODH-IN-3 (compound (S)-14d) is a potent, orally active dual inhibitor of RORγt (IC50: 0.098 μM) and DHODH (IC50: 0.432 μM) with significant in vivo anti-inflammatory effects.

RORγt DHODH-IN-1 (compound (R)-14d) is a potent, orally active dual inhibitor of RORγt (IC50: 0.083 μM) and DHODH (IC50: 0.172 μM), exhibiting significant in vivo anti-inflammatory effects.

RORγt inverse agonist 28 is a potent RORγt inverse agonist that regulates the differentiation of Th17 cells and inhibits IL-17 production, showing research potential in inflammatory and autoimmune diseases.

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

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