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ROR

The RAR-related orphan receptors (RORs) are members of the nuclear receptor family of intracellular transcription factors. There are three forms of ROR, ROR-α, -β, and -γ and each is encoded by a separate gene RORA, RORB, and RORC respectively. The RORs are somewhat unusual in that they appear to bind as monomers to hormone response elements as opposed to the majority of other nuclear receptors which bind as dimers. They bind to DNA elements called ROR response elements (RORE).

  • GSK805
    T73881426802-50-7
    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
    • $51
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    TargetMol | Inhibitor Hot
  • Cabozantinib hydrochloride
    T51641817759-42-4
    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).
    • $37
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  • ML 209
    T375871334526-14-5In house
    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.
    • $93
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  • XY101
    T133622349368-16-5In house
    XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).
    • $79
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  • AZD-0284
    T143692101291-07-8In house
    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].
    • $89
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  • Cholesterol
    T076057-88-5
    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.
    • $45
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    TargetMol | Citations Cited
  • Melatonin
    T165973-31-4
    Melatonin (Melatonine) is a biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.
    • $32
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  • RORγt inverse agonist 13
    T96232170477-75-3
    RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist (IC50=63.8 nM), with improved drug-like properties[1].
    • $98
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  • Bevurogant
    T392501817773-66-2
    Bevurogant is an antagonist of RORγt receptor and can be used in studies about the treatment of chronic inflammatory diseases.
    • $197
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  • RORγt inverse agonist 31
    T79470
    RORγt inverse agonist 31 (14g) is a potent antagonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an inhibitory concentration (IC50) of 0.428 μM. It has demonstrated efficacy in mitigating Imiquimod-induced psoriasis severity in murine models [1].
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  • T0901317
    T6690293754-55-9
    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).
    • $32
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    TargetMol | Citations Cited
  • TMP920
    T171081421837-45-7
    TMP920 inhibits RORγt binding to the SRC1 peptide (IC50: 0.03 μM). TMP920 is a highly potent and selective RORγt antagonist.
    • $119
    5 days
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  • SR0987
    T4670303126-97-8
    SR0987 is a RORγt agonist,
    • $64
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  • 3-Oxo-5β-cholanoic acid
    T135021553-56-6
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) (Dehydrolithocholic acid) is a bile acid metabolite and inhibits the differentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd: 1.13 μM).
    • $41
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  • TAK-828F
    T130671854901-94-2
    TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (IC50=1.9 nM, reporter gene IC50=6.1 nM).
    • $3,170
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  • RORγt Inverse agonist 8
    T127542079892-79-6
    RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM).
    • $1,670
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  • FM26
    T113082407981-35-3
    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.
    • $1,970
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  • TMP-778
    T13172L11422171-08-1
    TMP-778 is a selective inverse agonist of RORγt.
    • $223
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  • Cintirorgon
    TQ00072055536-64-4
    Cintirorgon (LYC-55716) is a selective, oral agonist of RORγ. Cintirorgon modulates gene expression of RORγ expressing T lymphocyte immune cells.
    • $77
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  • S18-000003
    T168322068119-11-7
    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.
    • $52
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  • RORγt inverse agonist 14
    T722522672496-70-5
    RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, exhibiting anti-inflammatory activity. It is employed in researching rheumatoid arthritis and psoriasis [1].
    • $1,770
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  • Vimirogant
    T167871802706-04-2
    Vimirogant is a RORγ inhibitor (Ki: <100 nM).
    • $2,270
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  • SR2211
    T169291359164-11-6
    SR2211 is a specific modulator and an inverse agonist of RORγ(IC50 = 320 nM, Ki = 105 nM).
    • $44
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  • SR3335
    T5160293753-05-6
    SR3335 (ML 176) is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).
    • $31
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  • RORγt Inverse agonist 6
    T127531887161-80-9
    RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.
    • $94
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  • RORγ antagonist 1
    T79464
    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].
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  • Nobiletin
    T2834478-01-3
    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).
    • $52
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    TargetMol | Citations Cited
  • Cedirogant
    T96352055496-11-0
    Cedirogant (ABBV-157) is an orally active retinoid-related orphan receptor-γt(RORγt) inverse agonist that is used for psoriasis study.
    • $128
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  • Methyl-3β-hydroxycholenate
    T1192320231-57-6
    Methyl-3β-hydroxycholenate (Methyl 3beta-hydroxychol-5-enoate) is a modulator of RORγ.
    • $1,520
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  • Zymostenol
    T35321566-97-2
    Zymostenol (5a-Cholest-8-en-3b-ol) is a RORγ agonist with an EC50 of 1 μM.Zymostenol is a late stage precursor of cholesterol biosynthesis.
    • $263
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  • TMP780
    T131721422053-03-9
    TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
    • $1,620
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  • A-9758
    T102102055271-22-0
    A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 drive
    • $2,570
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  • SR1078
    T45941246525-60-9
    SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.
    • $35
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    TargetMol | Citations Cited
  • GSK2981278
    T40501474110-21-8
    GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
    • $36
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  • SR1001
    T51631335106-03-0
    SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).
    • $34
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  • Neoruscogenin
    T3S125117676-33-4
    1. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.
    • $59
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