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Orphan Receptor

Orphan receptors refer to receptor proteins for which no endogenous ligands have yet been identified. They are widely found in superfamilies such as G protein-coupled receptors (GPCRs), nuclear receptors (NRs), and receptor tyrosine kinases (RTKs). These receptors possess a complete structure, including ligand-binding domains, transmembrane domains, and intracellular signalling domains; however, their functions remain poorly understood. They are often associated with embryonic development, metabolic regulation, inflammation, and tumourigenesis.

SID 7969543
SID7969543
T23354868224-64-0
SID 7969543 is a selective SF-1 inhibitor with potential anticancer activity, inhibits SF-1-triggered luciferase expression and can be used for cancer research.
  • $39
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AF64394
T84071637300-25-4
AF64394 is a selective inverse agonist of GPR3(pIC50 : 7.3)
  • $33
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TargetMol | Inhibitor Sale
TS-011
TS-011
T13215339071-18-0
N-(3-Chloro-4-morpholinophenyl)-N'-hydroxyformimidamide (TS-011) is a selective 20-Hydroxyeicosatetraenoic acid synthesis inhibitor.
  • $108
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RJW100
T386801276664-20-0In house
RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.
  • $247
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ML-180
SR1848
T12075863588-32-3
ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.
  • $30
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(Iso)-RJW100
T643631276664-61-9In house
(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.
  • $117
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BI-6015
T2186793987-29-2
BI 6015 is an antagonist of HNF4α. HNF4α is a nuclear receptor that regulates gene expression in the intestine cells, liver cells, and pancreas-β cells.
  • $34
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TargetMol | Citations Cited
CIA-1 (Free base)
CIA-1(Free base)
T71534L452087-38-6
CIA-1 (Free base) is a nuclear receptor COUP-TFII inhibitor with IC50 values ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines. CIA-1 (Free base) inhibits tumor growth in a mouse model of prostate cancer xenografts.
  • $31
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ML179
ML-179
T89541883548-87-5
ML179 is a potent and selective inverse agonist of liver receptor homolog-1 (LRH1, NR5A2) with IC50 of 320 nM.
  • $31
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DLPC
T2152018194-25-7
DLPC is an LRH-1 agonist ligand. DLPC is a phospholipid for biological study[1][2].
  • $39
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CID 1375606
CID-1375606, CID1375606
T5422313493-80-0
CID 1375606 is a surrogate agonist of the orphan G protein-coupled receptor [GPR27], characterized by a high level of conservation among vertebrates and predominant expression in the central nervous system.
  • $30
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LRH-1 Inhibitor-3
LRH-1-Inhibitor-3, LRH1 Inhibitor 3, LRH 1 Inhibitor 3
T257581185410-60-9
LRH-1 Inhibitor-3 is an antagonist that inhibits LRH-1 transcriptional activity, reducing the expression of target genes associated with cell growth and proliferation, such as SHP (small heterodimer partner), cyclin E1 (CCNE1), and G0S2, and inhibiting the proliferation of human pancreatic, colon, and breast adenocarcinoma cells.
  • $73
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NR2E3 agonist 1
T84349911211-69-3
NR2E3 agonist 1 is a small molecule photoreceptor-specific nuclear receptor (NR2E3) agonist with antitumor activity for the study of diseases caused by abnormalities in photoreceptor cell-specific receptors.
  • $81
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20-SOLA
T208783
20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.
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PSB-22269
T203177
PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.
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GPR61 Inverse agonist 1
T82263
Compound 1, identified as a GPR61 inverse agonist, exhibits an IC50 of 11 nM, rendering it suitable for metabolism and body weight disorder research, including obesity and cachexia [1].
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GPR34 receptor antagonist 3
T82264
Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1/2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].
  • $129
7-10 days
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Prolactin-Releasing Peptide (12-31), rat
T81391222988-10-5
Prolactin-Releasing Peptide (12-31), rat, a fragment of PrRP, exhibits high affinity for GPR10 receptors and stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor [1][2].
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Prosaptide TX14(A)
TP1970196391-82-9
Potent GPR37L1 and GPR37 agonist (EC50 values are 5 and 7 nM, respectively). Stimulates signaling through pertussis toxin-sensitive G proteins. Stimulates ERK phosphorylation. Protects against cellular stress. Promotes myelin lipid synthesis and prolongs
  • $823
35 days
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BMH-9
BMH 9
T23804457937-39-2
BMH-9 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.
  • $1,520
6-8 weeks
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Anticancer agent 258
T2031282891984-12-4
Anticanceragent 258 is an imidazo[1,2-B][1,2,4]triazole derivative that modulates nuclear receptor activity. It exhibits an EC50 of 63 nM for Nurr in N2A cells and an IC50 of 0.1 pM for Nur77 in HEK293 cells. Anticanceragent 258 is applicable in studies related to cancer, metabolic disorders, and neurological diseases.
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10-14 weeks
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SID7970631
T62757868224-75-3
SID7970631 is an isoquinolinone analogue, a selective and potent submicromolar SF-1 inhibitor with an IC50 of 260 nM. SID7970631 can be used to study cancer.
  • $766
6-8 weeks
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SS-RJW100
T61723
SS-RJW100 is an enantiomer of RJW100, known as a racemic agonist that targets two nuclear receptors: liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). In vitro experiments reveal that SS-RJW100 promotes the recruitment of coregulator protein fragments and enhances the interaction with the transcriptional intermediary factor 2 (Tif2) coactivator specifically for LRH-1. Additionally, SS-RJW100 disrupts the allosteric activation networks of LRH-1, displaying suboptimal thermal stability [1] [2].
  • $1,520
10-14 weeks
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NR2F1 agonist 1
T72776374101-64-1
NR2F1 agonist 1, a specific nuclear receptor NR2F1 activator, initiates dormancy programs in cancer cells by upregulating NR2F1 and its target genes controlling dormancy. This compound promotes neural crest-like features and suppresses growth in head and neck squamous cell carcinoma (HNSCC) through NR2F1 activation. Moreover, NR2F1 agonist 1 demonstrates tumor growth inhibition in a mouse primary tumor model.
  • $1,670
6-8 weeks
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