Search Result
Results for "
AHR antagonist 3
" in MCE Product Catalog:
3220
Inhibitors & Agonists
1
Biochemical Assay Reagents
346
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-147226
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- HY-145959
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- HY-145193
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- HY-103652
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- HY-144127
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AR antagonist 3
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Androgen Receptor
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Cancer
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AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.
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- HY-139708
-
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NMDA receptor antagonist-3
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iGluR
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Neurological Disease
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NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
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- HY-144286
-
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CXCR4 antagonist 3
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CXCR
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Infection
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CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus.
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- HY-151100
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GPR84 antagonist 3
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GPR84
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Inflammation/Immunology
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GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable.
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- HY-136152
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- HY-146026
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- HY-135773
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- HY-144419
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- HY-115912
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GPVI antagonist 3
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Others
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Cardiovascular Disease
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GPVI antagonist 3 (Compound 2) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 3 are, respectively, 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin and 51.74 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 3 is a promising antiplatelet agent.
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- HY-103649
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- HY-144372
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- HY-145919
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- HY-101264
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- HY-139874
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CXCR2 antagonist 3
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CXCR
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Cancer
Inflammation/Immunology
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CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues.
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- HY-142620
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- HY-144608
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Mu opioid receptor antagonist 3
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD).
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- HY-144139
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Estrogen receptor antagonist 3
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7).
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- HY-145124
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- HY-146456
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A1AR antagonist 3
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Adenosine Receptor
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Neurological Disease
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A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases.
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- HY-101915
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- HY-125820
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- HY-139904
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- HY-143315
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- HY-148076
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A2A receptor antagonist 3
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Adenosine Receptor
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Cancer
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A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.
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- HY-U00322
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- HY-138761
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- HY-137093
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- HY-147385
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CCR4 antagonist 3-1
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CCR
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Inflammation/Immunology
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CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [ 125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM).
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- HY-141609
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AHR antagonist 5 free base
|
Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.
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- HY-135830
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AHR antagonist 4
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Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects.
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- HY-135831
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AHR antagonist 2
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Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR.
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- HY-136220
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AHR antagonist 5
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Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
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- HY-136220A
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AHR antagonist 5 hemimaleate
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Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
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- HY-111449
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BAY-218
AHR antagonist 1
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Aryl Hydrocarbon Receptor
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Cancer
Inflammation/Immunology
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BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 μM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.
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- HY-144339
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AhR agonist 2
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Aryl Hydrocarbon Receptor
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Others
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AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis.
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- HY-135671
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- HY-118958
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Ablukast
Ro 23-3544
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Leukotriene Receptor
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Inflammation/Immunology
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Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. Ablukast effectively reduces LTC4- and antigen-induced bronchoconstriction. Ablukast is LTD4 receptor antagonist.
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- HY-50159
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- HY-17357
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- HY-B0678
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- HY-17357S
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Nepafenac-d5
AHR-9434-d5; AL-6515-d5
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COX
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Others
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Nepafenac D5 (AHR-9434 D5) is the deuterium labeled Nepafenac, which is a selective COX-2 inhibitor.
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- HY-147544
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- HY-147543
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- HY-147545
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- HY-135829
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BAY 2416964
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Aryl Hydrocarbon Receptor
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Cancer
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BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
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- HY-144733
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- HY-129995A
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- HY-12908
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Bcl-xL antagonist 2
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).
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- HY-147808
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- HY-148038
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5-HT3 antagonist 5
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5-HT Receptor
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Neurological Disease
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5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice.
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- HY-130270
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- HY-147203
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- HY-143314
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- HY-147222
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SAE-14
GPR183 antagonist-1
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EBI2/GPR183
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Inflammation/Immunology
Neurological Disease
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SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice.
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- HY-139643A
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CXCR7 antagonist-1 hydrochloride
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CXCR
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Cancer
Inflammation/Immunology
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CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).
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- HY-139643
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CXCR7 antagonist-1
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CXCR
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Cancer
Inflammation/Immunology
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CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).
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- HY-W014502
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D-Kynurenine
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Aryl Hydrocarbon Receptor
Endogenous Metabolite
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Cancer
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D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
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- HY-101745
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- HY-143313
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- HY-B0845
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- HY-122208
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SGA360
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Others
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Inflammation/Immunology
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SGA360 suppress inflammatory SAA1 signaling in an AHR-dependent manner through a mechanism that does not require AHR binding to its cognate response element (partial antagonist).
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- HY-102023
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GNF351
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Aryl Hydrocarbon Receptor
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Others
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GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
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- HY-118780
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- HY-117102
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ANI-7
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Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
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Cancer
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ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
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- HY-15015A
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- HY-111500
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- HY-111500A
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- HY-15015
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- HY-103220
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- HY-147762
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- HY-112264
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- HY-103650
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- HY-144377
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- HY-15001
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- HY-U00320
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- HY-U00330
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- HY-112262
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- HY-144383
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RXR antagonist 2
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RAR/RXR
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Others
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RXR antagonist 2 (compound 6b) is a potent antagonist of RXR with a Ki and Kd of 0.391 and 0.281 μM. RXR antagonist 2 has the potential for the research of RXR related diseases.
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- HY-144390
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GPVI antagonist 1
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Others
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Cardiovascular Disease
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GPVI antagonist 1 (compound 5) is a glycoprotein VI (GPVI) platelet receptor antagonist. GPVI antagonist 1 inhibits collagen-induced platelet aggregation with an IC50 of 25.3 μM.
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- HY-136437
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- HY-112562
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- HY-103651
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- HY-134864
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- HY-112265
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- HY-18075
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- HY-101536
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- HY-147392
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- HY-132936
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- HY-146405
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- HY-U00334
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- HY-U00375
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- HY-145451
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- HY-133034
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- HY-131337
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RhlR antagonist 1
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Bacterial
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Infection
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RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections.
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- HY-136922
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- HY-P1185
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Antagonist G
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Vasopressin Receptor
Apoptosis
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Cancer
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Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
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- HY-139675
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- HY-U00331
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- HY-139873
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- HY-112263
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- HY-146101
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- HY-151391
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LPA5 antagonist 1
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Others
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Neurological Disease
|
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LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research.
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- HY-151481
-
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FXR antagonist 1
|
FXR
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Metabolic Disease
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FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies.
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- HY-115911
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GPVI antagonist 2
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Others
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Cardiovascular Disease
|
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GPVI antagonist 2 (Compound 1) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 2 are, respectively, 0.35 μM for collagen, 0.80 μM for CRP, 195.2 μM for convulxin and 81.38 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 2 is a promising antiplatelet agent.
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- HY-111443
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- HY-112792
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- HY-100331
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- HY-147979
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CXCR4 antagonist 9
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CXCR
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Cancer
Infection
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CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM.
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- HY-100321
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- HY-147978
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CXCR4 antagonist 8
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CXCR
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Cancer
Infection
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CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration.
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- HY-144780
-
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CXCR2 antagonist 4
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CXCR
|
Cancer
|
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CXCR2 antagonist 4 (compound 7) is a potent CXCR2 antagonist with an IC50 value of 0.13 μM. CXCR2 antagonist 4 can inhibit CXCL8-induced cytosolic calcium increase (IC50 = 27 μM). CXCR2 antagonist 4 can be used for researching anticancer.
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- HY-146401
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CXCR4 antagonist 6
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CXCR
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Cancer
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CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice.
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- HY-U00359
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- HY-143253
-
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Estrogen receptor antagonist 7
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities.
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- HY-146027
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Androgen receptor antagonist 4
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities.
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- HY-144197
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- HY-126217
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- HY-151392
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- HY-151247
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GnRH-R antagonist 1
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GnRH Receptor
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Cancer
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GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
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- HY-142923
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AR antagonist 2
|
Androgen Receptor
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Cancer
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AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research.
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- HY-112430
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- HY-111494
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-
- HY-125970
-
-
- HY-145697
-
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GPR84 antagonist 2
|
GPR84
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Inflammation/Immunology
|
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GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis.
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- HY-136459
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NMDA receptor antagonist 2
|
iGluR
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Neurological Disease
|
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NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
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- HY-151435
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CCR6 antagonist 1
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CCR
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Inflammation/Immunology
|
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CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs).
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- HY-107551
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GLI antagonist-1
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Gli
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Cancer
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GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner.
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- HY-146494
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Androgen receptor antagonist 5
|
Androgen Receptor
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Cancer
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Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer.
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- HY-12545
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Brevetoxin-3
PbTx-3
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Sodium Channel
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Inflammation/Immunology
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Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
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- HY-114193
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- HY-114194
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- HY-130261
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-
- HY-100261
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-
- HY-144064
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- HY-113973
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LPA2 antagonist 2
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LPL Receptor
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Cancer
|
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LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
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- HY-136645
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- HY-138501
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- HY-144784
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- HY-144781
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-
- HY-144609
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Mu opioid receptor antagonist 4
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Opioid Receptor
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Neurological Disease
|
|
Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD).
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- HY-U00408
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-
- HY-144783
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- HY-103222
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DiMNF
3',4'-Dimethoxy-αNF
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Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
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DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent.
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- HY-124759
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- HY-144202
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Estrogen receptor antagonist 4
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Estrogen Receptor/ERR
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Cancer
|
|
Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1).
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- HY-130845
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- HY-129636
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(E)-GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- HY-146517
-
-
- HY-18076
-
-
- HY-100170
-
-
- HY-114017
-
-
- HY-U00397
-
-
- HY-151266
-
|
AR antagonist 4
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM.
|
-
- HY-144137
-
|
Estrogen receptor antagonist 1
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4).
|
-
- HY-143563
-
|
NLRP3 antagonist 1
|
NOD-like Receptor (NLR)
|
Cancer
|
|
NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3).
|
-
- HY-P1185A
-
-
- HY-146372
-
|
CXCR4 antagonist 5
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately.
|
-
- HY-144204
-
|
Estrogen receptor antagonist 5
|
Estrogen Receptor/ERR
|
Cancer
Endocrinology
|
|
Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165).
|
-
- HY-144206
-
|
Estrogen receptor antagonist 6
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166).
|
-
- HY-151387
-
|
A2AAR antagonist 1
|
Others
|
Neurological Disease
|
|
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases.
|
-
- HY-U00368
-
-
- HY-147379
-
|
Hepcidin antagonist-1
|
Others
|
Metabolic Disease
|
|
Hepcidin antagonist-1 (example 104) is a potent hepcidin (hepcidine) antagonist with an IC50<50 μM. Hepcidin antagonist-1 can be used for researching iron metabolism disorders, such as anemias.
|
-
- HY-147557
-
|
PAC1R antagonist 1
|
Others
|
Neurological Disease
|
|
PAC1R antagonist 1 (compound 3d) is a potent and orally active antagonist of PAC1 receptor. PAC1R antagonist 1 can inhibit pituitary adenylate cyclase-activating polypeptide (PACAP)- and nerve injury-induced allodynia.
|
-
- HY-146457
-
-
- HY-100274
-
-
- HY-U00353
-
-
- HY-130992
-
-
- HY-129357
-
-
- HY-112629
-
-
- HY-114097A
-
|
CCR1 antagonist 11 hydrochloride
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC50 values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases.
|
-
- HY-147506
-
|
NOD2 antagonist 1
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs.
|
-
- HY-13499
-
|
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.
|
-
- HY-144607
-
|
Mu opioid receptor antagonist 2
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
|
-
- HY-141865
-
-
- HY-146289
-
|
LXR antagonist 2
|
LXR
|
Metabolic Disease
|
|
LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, with IC50 values of 0.36 and 2.25 μM for LXRβ and LXRα, respectively. LXR antagonist 2 is a lipogenesis inhibitor through down-regulating LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 shows lipid-lowering effects in mice with Triton WR-1339-induced hyperlipidemia.
|
-
- HY-146410
-
|
AT2R antagonist 1
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common drug-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.
|
-
- HY-141845
-
-
- HY-144610
-
|
Mu opioid receptor antagonist 5
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).
|
-
- HY-115745
-
|
Calmodulin antagonist-1
|
Calmodulin
|
Cardiovascular Disease
|
|
Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=28 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=375 μM) in a competitive fashion with respect to cyclic GMP and the Ki value is 300 μM.
|
-
- HY-18619
-
|
YL-109
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
|
-
- HY-U00365
-
-
- HY-101913
-
-
- HY-136905
-
-
- HY-102037
-
-
- HY-125836
-
|
CCR4 antagonist 2
|
CCR
|
Cancer
Endocrinology
|
|
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
|
-
- HY-12684
-
|
CH-223191
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR).
CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
|
-
- HY-114191B
-
-
- HY-144699
-
|
ERRα antagonist-2
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.
|
-
- HY-146383
-
|
H3R antagonist 2
|
Histamine Receptor
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB.
|
-
- HY-144200
-
|
CCR8 antagonist 2
|
CCR
|
Cancer
Neurological Disease
|
|
CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the treatment of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220).
|
-
- HY-150692
-
|
Estrogen receptor α antagonist 1
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer.
|
-
- HY-146220
-
-
- HY-146272
-
-
- HY-148259
-
|
SF-1 antagonist-1
|
Others
|
Cancer
|
|
SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer.
|
-
- HY-114191
-
-
- HY-143568
-
-
- HY-111501
-
-
- HY-147132
-
|
GluR6 antagonist-1
|
iGluR
|
Neurological Disease
|
|
GluR6 antagonist-1 is a benzothiophene derivative, acting as a GluR6 antagonist. GluR6 antagonist-1 can be used for researching acute and chronic neurological disorders.
|
-
- HY-U00286
-
-
- HY-146588
-
|
NMDA receptor antagonist 4
|
iGluR
Others
|
Neurological Disease
|
|
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
|
-
- HY-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- HY-135270
-
-
- HY-13232
-
|
ITK antagonist
|
Itk
|
Inflammation/Immunology
|
|
ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM.
|
-
- HY-144606
-
|
Mu opioid receptor antagonist 1
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC).
|
-
- HY-150693
-
-
- HY-146436
-
-
- HY-144285
-
|
CXCR4 antagonist 4
|
CXCR
HIV
|
Inflammation/Immunology
|
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
|
-
- HY-145195
-
-
- HY-146431
-
-
- HY-U00321
-
-
- HY-139677
-
-
- HY-145192
-
-
- HY-145191
-
-
- HY-112659
-
|
Lin28-let-7 antagonist 1
|
Others
|
Cancer
Neurological Disease
|
|
Lin28-let-7 antagonist 1 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction. Lin28-let-7 antagonist 1 inhibits Lin28A binding to pre-let-7a-2, with an IC50 of 8 μM. Lin28-let-7 antagonist 1 inhibits proliferation in human cancer cells.
|
-
- HY-147106
-
-
- HY-133123
-
-
- HY-145886
-
|
TLR7/8 antagonist 1
|
Toll-like Receptor (TLR)
|
Cancer
Infection
Inflammation/Immunology
|
|
TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.
|
-
- HY-144672
-
-
- HY-145194
-
-
- HY-101116
-
|
GLP-1R Antagonist 1
|
GCGR
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
|
-
- HY-144116
-
-
- HY-144138
-
|
Estrogen receptor antagonist 2
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3).
|
-
- HY-143576
-
-
- HY-114191A
-
-
- HY-115974
-
|
GRPR antagonist-1
|
Others
|
Cancer
|
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.
|
-
- HY-145468
-
|
GPR52 antagonist-1
|
Others
|
Neurological Disease
|
|
GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons.
|
-
- HY-116649
-
-
- HY-101695
-
-
- HY-145893
-
-
- HY-145892
-
-
- HY-P2268
-
|
RAGE antagonist peptide
|
Amyloid-β
|
Cancer
Inflammation/Immunology
|
|
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities.
|
-
- HY-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-101704
-
-
- HY-125821
-
|
Sigma-1 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
|
-
- HY-115975
-
|
GRPR antagonist-2
|
Others
|
Cancer
|
|
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.
|
-
- HY-125819
-
-
- HY-144603
-
-
- HY-145684
-
-
- HY-145905
-
-
- HY-135976
-
|
P2X3 antagonist 34
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
|
-
- HY-139314
-
-
- HY-111669
-
-
- HY-114025
-
-
- HY-150068
-
-
- HY-108323
-
|
CCR2 antagonist 4
Teijin compound 1
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-103362
-
|
CCR2 antagonist 4 hydrochloride
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-139677A
-
-
- HY-137175
-
|
TMBIM6 antagonist-1
|
mTOR
|
Cancer
|
|
TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+.
|
-
- HY-U00382
-
-
- HY-133555
-
-
- HY-144619
-
|
TLR7/8 antagonist 2
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
|
-
- HY-P2268A
-
|
RAGE antagonist peptide TFA
|
Amyloid-β
|
Cancer
Inflammation/Immunology
|
|
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities.
|
-
- HY-102051
-
|
XIAP/cIAP1 antagonist-1
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
|
-
- HY-134542
-
|
CaV1.3 antagonist-1
|
Calcium Channel
|
Neurological Disease
|
|
CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research.
|
-
- HY-106659
-
-
- HY-101802
-
-
- HY-U00010
-
-
- HY-131868
-
|
TRPV3 antagonist 74a
|
TRP Channel
|
Neurological Disease
|
|
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain.
|
-
- HY-146478
-
|
A1/A3 AR antagonist 1
|
Adenosine Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
|
-
- HY-146034
-
|
NOD1/2 antagonist-1
|
NOD-like Receptor (NLR)
|
Cancer
Inflammation/Immunology
|
|
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).
|
-
- HY-102024
-
-
- HY-148252
-
|
ADRA1D receptor antagonist 1 free base
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-147398
-
-
- HY-144764
-
-
- HY-107698
-
-
- HY-100692
-
|
Lin28-let-7a antagonist 1
|
MicroRNA
|
Cancer
|
|
Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
|
-
- HY-144115
-
-
- HY-112219A
-
-
- HY-129995
-
|
TSHR antagonist S37b
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
|
-
- HY-146479
-
-
- HY-145106
-
-
- HY-10815
-
-
- HY-150059
-
-
- HY-146486
-
|
P2Y2R/GPR17 antagonist 1
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-109147A
-
-
- HY-101622
-
-
- HY-110203
-
|
R-7050
TNF-α antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- HY-16692
-
-
- HY-120588
-
-
- HY-147707
-
|
CB2 receptor antagonist 1
|
Cannabinoid Receptor
|
Others
|
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
|
-
- HY-129946
-
-
- HY-139680
-
-
- HY-139681
-
-
- HY-P3232
-
-
- HY-19317
-
-
- HY-145706
-
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
|
-
- HY-145466
-
|
EVT-401
P2X7 receptor antagonist-1
|
P2X Receptor
|
Neurological Disease
|
|
EVT-401 (P2X7 receptor antagonist-1) is a purinergic P2X7 receptor antagonist. EVT-401 has efficacy of combating neuroinflammation.
|
-
- HY-104026B
-
-
- HY-131016
-
|
IHR-Cy3
|
Smo
|
Cancer
|
|
IHR-Cy3 is a potent fluorescent Smo antagonist with an IC50 of 100 nM.
|
-
- HY-145862
-
-
- HY-107031
-
|
Metapramine
19560 RP
|
iGluR
Others
|
Others
|
|
Metapramine (19560 RP) is an antidepressant agent, belonging to the class of tricyclic compounds. Metapramine inhibits norepinephrine reuptake, without affecting the reuptake of serotonin or dopamine. Metapramine is a low-affinity antagonist of the N-methyl-D-aspartic acid (NMDA) receptor complex channel.
|
-
- HY-114740
-
-
- HY-103009
-
|
MSX-127
|
CXCR
|
Cancer
|
|
MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
|
-
- HY-103010
-
|
MSX-130
|
CXCR
|
Cancer
|
|
MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
|
-
- HY-N4095
-
-
- HY-112050
-
-
- HY-122136
-
|
S26131
|
Melatonin Receptor
|
Neurological Disease
|
|
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
|
-
- HY-A0125
-
-
- HY-147541
-
-
- HY-107327
-
|
Carazolol
(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist.
|
-
- HY-108530
-
|
MM11253
|
RAR/RXR
|
Cancer
|
|
MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.
|
-
- HY-12451
-
-
- HY-P1276
-
-
- HY-14794
-
|
Dextromilnacipran
(1R,2S)-milnacipran; F2696
|
Serotonin Transporter
|
Metabolic Disease
|
|
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-113329
-
|
Guanidinoethyl sulfonate
Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats. Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport.
|
-
- HY-100242
-
-
- HY-N10123
-
-
- HY-110303
-
-
- HY-N0178
-
-
- HY-135750
-
|
VAF347
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
|
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
|
-
- HY-111441
-
-
- HY-P1276A
-
-
- HY-112627
-
-
- HY-133112
-
-
- HY-107537
-
-
- HY-100452A
-
-
- HY-107611
-
-
- HY-133533
-
|
O-2050
|
Cannabinoid Receptor
|
Neurological Disease
|
|
O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice.
|
-
- HY-120629
-
|
BMS-639623
|
CCR
|
Inflammation/Immunology
|
|
BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma.
|
-
- HY-111186
-
-
- HY-105689
-
|
AGN 192870
|
RAR/RXR
|
Others
|
|
AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism.
|
-
- HY-B1067A
-
-
- HY-108480
-
-
- HY-100382
-
|
FPTQ
|
mGluR
|
Others
|
|
FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
|
-
- HY-103223
-
|
Phortress
NSC 710305
|
Cytochrome P450
|
Cancer
|
|
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
|
-
- HY-130256
-
|
β-NF-JQ1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
|
-
- HY-N10397
-
|
Maceneolignan H
|
CCR
|
Inflammation/Immunology
|
|
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases.
|
-
- HY-146809
-
|
Galectin-3 antagonist 2
|
Galectin
|
Cancer
|
|
Galectin-3 is a β Galactoside specific carbohydrate recognition protein (lectin) has the ability to promote the migration of B cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and withstand drug therapy.
|
-
- HY-141411
-
|
(Rac)-Zevaquenabant
(Rac)-MRI-1867
|
Cannabinoid Receptor
NO Synthase
|
Others
|
|
(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoid receptor type 1 (CB1R)/iNOS antagonist, with a Ki of 5.7 nM for CB1R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis.
|
-
- HY-109044
-
-
- HY-105790
-
|
Piperilate
Pipethanate
|
Cholinesterase (ChE)
|
Others
|
|
Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates.
|
-
- HY-13204
-
|
Biperiden hydrochloride
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-13204A
-
|
Biperiden
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-135147
-
|
ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-150067
-
|
CB1R antagonist 1
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity.
|
-
- HY-119401
-
|
CAY10444
BML-241
|
LPL Receptor
|
Cancer
|
|
CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors.
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-13204B
-
|
Biperiden lactate
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-16489
-
|
Terodiline
|
Potassium Channel
mAChR
Calcium Channel
|
Metabolic Disease
|
|
Terodiline, an antispasmodic agent, blocks hERG current with the IC50 of 375 nM. Terodiline has both anticholinergic and calcium antagonist properties, and effectively reduces abnormal bladder contractions caused by detrusor instability. Terodiline can be used for the research of urinary incontinence.
|
-
- HY-111321
-
-
- HY-14431
-
|
Cerlapirdine
SAM-531; PF-05212365
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
|
-
- HY-16474
-
|
Relugolix
TAK-385
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
|
-
- HY-N10295
-
|
Flavipin
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4 + T cells and CD11b + macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM.
|
-
- HY-150790
-
-
- HY-15484
-
-
- HY-50848
-
|
BW A868C
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP).
|
-
- HY-151413
-
-
- HY-14407
-
-
- HY-B1690
-
-
- HY-B1690A
-
-
- HY-14407A
-
-
- HY-149014
-
-
- HY-146413
-
|
HF50731
|
CXCR
HIV
|
Cancer
Infection
|
|
HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM.
|
-
- HY-12028
-
|
PD98059
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
|
-
- HY-108683
-
|
ACT-335827
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.
|
-
- HY-N6264
-
-
- HY-N0586A
-
|
Norisoboldine hydrochloride
(+)-Laurelliptine hydrochloride
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
|
-
- HY-16031
-
-
- HY-N0586
-
|
Norisoboldine
(+)-Laurelliptine
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
|
-
- HY-P3245
-
|
HXR9
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.
|
-
- HY-P3245A
-
|
HXR9 hydrochloride
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.
|
-
- HY-12397
-
|
ZK159222
|
VD/VDR
|
Endocrinology
|
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
|
-
- HY-145341
-
|
GNE-149
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
|
-
- HY-N6932
-
-
- HY-116248
-
|
Ro 41-5253
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.
|
-
- HY-B0311A
-
|
Carbidopa monohydrate
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-B0311
-
|
Carbidopa
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-109593
-
-
- HY-N0170
-
-
- HY-W028393
-
-
- HY-123012
-
|
Lubabegron
LY-488756
|
Adrenergic Receptor
|
Others
|
|
Lubabegron is a potent modulator of β-adrenergic receptor (β -AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste.
|
-
- HY-103221
-
-
- HY-150751
-
|
ODN TTAGGG
ODN A151
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
|
-
- HY-110206
-
|
AM6545
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications.
|
-
- HY-103454B
-
|
MPP hydrochloride
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
|
-
- HY-17038A
-
|
Agomelatine hydrochloride
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038
-
|
Agomelatine
S-20098
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038B
-
-
- HY-14117
-
-
- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
Apoptosis
|
Cancer
Neurological Disease
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
|
-
- HY-108608
-
|
o-3M3FBS
|
Others
|
Others
|
|
o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca 2+]i in an agonistic manner.
|
-
- HY-19826
-
-
- HY-12709A
-
-
- HY-19037
-
|
SM-2470
|
Adrenergic Receptor
|
Metabolic Disease
Neurological Disease
|
|
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats. SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization.
|
-
- HY-146446
-
|
PXYC1
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).
|
-
- HY-146451
-
|
PXYC12
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC12 is a ribosomal protein S1 (RpsA) antagonist with Kds of 2.67 and 4.67 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).
|
-
- HY-146450
-
|
PXYC2
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC2 is a ribosomal protein S1 (RpsA) antagonist with Kds of 6.35 and 5.11 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).
|
-
- HY-146447
-
|
PXYC13
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC13 is a ribosomal protein S1 (RpsA) antagonist with Kds of 7.61 and 8.50 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).
|
-
- HY-146449
-
|
PXYD4
|
Bacterial
Antibiotic
|
Infection
|
|
PXYD4 is a ribosomal protein S1 (RpsA) antagonist with Kds of 3.24 and 1.64 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).
|
-
- HY-130842
-
-
- HY-B0311AS
-
|
Carbidopa-d3 monohydrate
(S)-(-)-Carbidopa-d3 monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa-d3 ((S)-(-)-Carbidopa-d3) monohydrate is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-147560
-
-
- HY-101283
-
|
HCH6-1
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
|
-
- HY-131340
-
|
LASSBio-1632
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.
|
-
- HY-P3678
-
-
- HY-145258
-
-
- HY-115450
-
|
ONO-0300302
|
LPL Receptor
|
Cancer
Endocrinology
|
|
ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research.
|
-
- HY-147280
-
|
Misetionamide
|
Apoptosis
|
Cancer
|
|
Misetionamide is an orally oxathiazin-like compound. Misetionamide is a glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with antineoplastic activity. Misetionamide can be used for the research of cancer.
|
-
- HY-134983
-
-
- HY-124421
-
|
5F-203
NSC-703786
|
Aryl Hydrocarbon Receptor
|
Others
|
|
5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38.
|
-
- HY-119873
-
|
Celiprolol
REV 5320
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
|
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
|
-
- HY-A0083
-
|
Methacholine chloride
Acetyl-β-methylcholine chloride
|
mAChR
|
Others
|
|
Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-A0083B
-
|
Methacholine bromide
Acetyl-β-methylcholine bromide
|
mAChR
|
Cardiovascular Disease
|
|
Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-W011338
-
|
Benzyl butyl phthalate
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
|
-
- HY-103575A
-
|
MFZ 10-7 hydrochloride
|
mGluR
|
Neurological Disease
|
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
|
-
- HY-10036
-
-
- HY-50158
-
-
- HY-10341
-
|
Fasudil Hydrochloride
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341C
-
|
Fasudil dihydrochloride
HA-1077 dihydrochloride; AT-877 dihydrochloride
|
Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341A
-
|
Fasudil
HA-1077; AT877
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-10341B
-
|
Fasudil hydrochloride semihydrate
HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
|
ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-121885
-
|
LMD-009
|
CCR
|
Metabolic Disease
Endocrinology
|
|
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
|
-
- HY-145906
-
|
D4R antagonis-2
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.
|
-
- HY-147273
-
-
- HY-109196
-
-
- HY-147417S
-
-
- HY-119019
-
-
- HY-147294
-
-
- HY-128781
-
|
Glucagon receptor antagonists-5
|
GCGR
|
Metabolic Disease
|
|
Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM).
|
-
- HY-106561
-
-
- HY-100814
-
-
- HY-100535
-
-
- HY-100122
-
-
- HY-110240
-
-
- HY-22437
-
-
- HY-118844
-
-
- HY-125145
-
-
- HY-U00121
-
-
- HY-106416
-
-
- HY-P1782
-
-
- HY-B1439B
-
-
- HY-50713
-
-
- HY-114427
-
-
- HY-B0918
-
-
- HY-107430
-
|
Oxythiamine
Hydroxythiamin
|
Others
|
Cancer
|
|
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
|
-
- HY-110037
-
-
- HY-P3450
-
-
- HY-100471
-
-
- HY-146404
-
-
- HY-108972
-
-
- HY-13209C
-
-
- HY-117793
-
-
- HY-107706
-
-
- HY-15257A
-
-
- HY-121186
-
-
- HY-124300A
-
-
- HY-104059
-
-
- HY-B0548S1
-
-
- HY-117153
-
-
- HY-111484
-
-
- HY-70002B
-
-
- HY-N1163
-
-
- HY-N3610
-
|
Coclaurine
|
nAChR
|
Neurological Disease
|
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
|
-
- HY-A0027S
-
-
- HY-101139
-
-
- HY-112248
-
-
- HY-116263
-
-
- HY-15540
-
-
- HY-P2165
-
-
- HY-18668
-
-
- HY-22437S
-
-
- HY-B2111
-
-
- HY-108396
-
-
- HY-22437S1
-
-
- HY-100913
-
-
- HY-100648
-
-
- HY-100649
-
-
- HY-15066
-
|
CNQX
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
|
-
- HY-14656S
-
-
- HY-B1296S
-
-
- HY-135500
-
-
- HY-100248
-
-
- HY-U00067
-
-
- HY-101685
-
-
- HY-112056
-
-
- HY-15277
-
-
- HY-101638
-
-
- HY-14656S1
-
-
- HY-19638A
-
|
Cangrelor tetrasodium
AR-C69931MX tetrasodium
|
P2Y Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
|
-
- HY-B0524A
-
-
- HY-148179
-
-
- HY-131449
-
-
- HY-D0237
-
-
- HY-B0524
-
-
- HY-12503
-
-
- HY-12195
-
-
- HY-15066A
-
|
CNQX disodium
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
|
-
- HY-16991
-
-
- HY-B1547A
-
-
- HY-100266
-
-
- HY-19223
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-U00017
-
-
- HY-19818A
-
-
- HY-145234
-
-
- HY-19705B
-
-
- HY-N2189
-
-
- HY-19638
-
|
Cangrelor
AR-C69931MX
|
P2Y Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist.
|
-
- HY-16346S
-
-
- HY-128878
-
-
- HY-13242
-
|
Taladegib
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
-
- HY-15372
-
-
- HY-106910
-
-
- HY-100280
-
-
- HY-B1589A
-
-
- HY-B1014
-
-
- HY-101574
-
-
- HY-101594
-
-
- HY-U00062
-
-
- HY-101675
-
-
- HY-101707
-
-
- HY-B1240
-
-
- HY-105117
-
-
- HY-17039S
-
-
- HY-G0014
-
|
Quetiapine sulfoxide
Quetiapine S-oxide
|
Drug Metabolite
|
Neurological Disease
|
|
Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.
|
-
- HY-G0014B
-
-
- HY-70050AS
-
-
- HY-G0014A
-
-
- HY-W025443
-
-
- HY-14277A
-
|
Levocabastine hydrochloride
R 50547 hydrochloride
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
|
-
- HY-14277
-
|
Levocabastine
R 50547
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
|
-
- HY-B1808
-
|
Triprolidine
|
Histamine Receptor
|
Infection
|
|
Triprolidine is an orally active H1R Antagonist antagonist. Triprolidine has the function of spinal cord motor and sensory block. Triprolidine can be used for the research of allergic rhinitis.
|
-
- HY-107603
-
|
NS3763
|
iGluR
|
Neurological Disease
|
|
NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors.
|
-
- HY-P0107
-
-
- HY-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-101534
-
-
- HY-145611
-
-
- HY-U00247
-
-
- HY-B0768A
-
-
- HY-U00245
-
-
- HY-13202
-
-
- HY-U00202
-
-
- HY-B0460
-
-
- HY-100173
-
-
- HY-100903
-
-
- HY-B1165
-
-
- HY-U00110
-
-
- HY-103531
-
-
- HY-B0325
-
-
- HY-U00119
-
-
- HY-101691
-
-
- HY-B1303A
-
-
- HY-13209
-
-
- HY-110254
-
-
- HY-B2154
-
-
- HY-131256A
-
-
- HY-B0561
-
-
- HY-131256
-
-
- HY-12966
-
-
- HY-100649S
-
-
- HY-P1025
-
-
- HY-B1438
-
-
- HY-N2079
-
-
- HY-N6628
-
-
- HY-U00234
-
-
- HY-145610
-
-
- HY-100255
-
-
- HY-110110
-
-
- HY-U00139
-
-
- HY-U00350
-
-
- HY-A0250
-
-
- HY-B2168
-
-
- HY-100454
-
-
- HY-112620
-
-
- HY-B1283
-
-
- HY-B1303
-
-
- HY-100668
-
-
- HY-100292
-
-
- HY-15539
-
-
- HY-101743
-
-
- HY-B0286A
-
-
- HY-B1164
-
-
- HY-17465
-
-
- HY-100191
-
-
- HY-14276A
-
|
Gallopamil hydrochloride
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-B0524AS
-
-
- HY-14276
-
|
Gallopamil
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-100798
-
|
Phaclofen
|
GABA Receptor
|
Neurological Disease
|
|
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
|
-
- HY-108069
-
-
- HY-P0107A
-
-
- HY-112730
-
|
PEO-IAA
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-145257
-
-
- HY-17369AS
-
|
Tirofiban-d9 hydrochloride
L700462-d9 hydrochloride; MK383-d9 hydrochloride
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban-d9 (L700462-d9) hydrochloride is the deuterium labeled Tirofiban. Tirofiban(L700462) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.
|
-
- HY-P3808
-
-
- HY-A0019S
-
|
Paliperidone-d4
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-14778
-
-
- HY-110097
-
-
- HY-109171
-
-
- HY-115874
-
-
- HY-15085
-
-
- HY-145553
-
-
- HY-19732
-
-
- HY-16763
-
-
- HY-B0009
-
-
- HY-10164
-
-
- HY-101632
-
-
- HY-U00019
-
-
- HY-101600
-
-
- HY-101602
-
-
- HY-101618
-
-
- HY-15073
-
-
- HY-B0895
-
-
- HY-18101A
-
-
- HY-124157
-
-
- HY-U00040
-
-
- HY-P1396A
-
-
- HY-102004
-
-
- HY-108555
-
-
- HY-N0096
-
-
- HY-B1487
-
|
Procyclidine hydrochloride
Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
|
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-B1487A
-
|
Procyclidine
Tricyclamol; (±)-Procyclidine
|
mAChR
iGluR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-42849
-
-
- HY-15487
-
-
- HY-13021
-
-
- HY-17582
-
-
- HY-145297
-
-
- HY-109147
-
-
- HY-10304
-
-
- HY-19737A
-
-
- HY-101502A
-
-
- HY-12710A
-
-
- HY-16509
-
-
- HY-107602
-
-
- HY-112703
-
-
- HY-14538A
-
-
- HY-P0061
-
-
- HY-13439
-
-
- HY-12114
-
-
- HY-50663
-
-
- HY-42849A
-
-
- HY-109077
-
-
- HY-101797
-
-
- HY-A0066
-
-
- HY-15758
-
-
- HY-U00018
-
-
- HY-19243
-
-
- HY-101668
-
-
- HY-19163
-
-
- HY-103099
-
-
- HY-100153
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-14538
-
-
- HY-B1416A
-
-
- HY-12881
-
|
Eliprodil
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-102094
-
|
(E/Z)-SIB-1893
|
mGluR
|
Neurological Disease
|
|
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist.
|
-
- HY-103476
-
|
Ro15-4513
|
GABA Receptor
|
Neurological Disease
|
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
|
-
- HY-126068
-
-
- HY-N0607
-
-
- HY-13706A
-
|
CAY10471
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.
|
-
- HY-A0163S
-
-
- HY-100405
-
|
FTIDC
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
|
-
- HY-B0549A
-
|
Flavoxate hydrochloride
Rec-7-0040; DW61
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
|
-
- HY-111616
-
|
GSK1820795A
|
PPAR
Angiotensin Receptor
|
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides. GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38).
|
-
- HY-A0019A
-
|
Paliperidone palmitate
9-Hydroxyrisperidone palmitate
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.
|
-
- HY-A0066A
-
-
- HY-108458
-
-
- HY-76520
-
-
- HY-15709
-
-
- HY-100850
-
-
- HY-110095
-
-
- HY-18697
-
-
- HY-112604
-
-
- HY-15574
-
-
- HY-19768
-
-
- HY-102093
-
-
- HY-109074
-
-
- HY-143518
-
-
- HY-142868
-
-
- HY-16732
-
-
- HY-U00363
-
-
- HY-A0075
-
-
- HY-A0145
-
|
Phenprocoumon
|
Others
|
Others
|
|
Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
|
-
- HY-16701
-
|
BV6
|
IAP
|
Cancer
|
|
BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
|
-
- HY-12510
-
-
- HY-15574A
-
-
- HY-P0264
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-101706
-
-
- HY-101830
-
-
- HY-101721
-
-
- HY-50912
-
-
- HY-P0209
-
-
- HY-U00283
-
-
- HY-15702
-
|
HJC0350
|
Others
|
Cancer
|
|
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
|
-
- HY-19973
-
-
- HY-G0012
-
-
- HY-U00404
-
-
- HY-U00188
-
-
- HY-U00207
-
-
- HY-50691
-
-
- HY-B0561S2
-
-
- HY-U00449G
-
|
AGN 193109
|
RAR/RXR
|
Cancer
|
|
AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist.
|
-
- HY-B0524AS1
-
-
- HY-100607A
-
-
- HY-B0549
-
|
Flavoxate
Rec-7-0040 free base; DW61 free base
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
|
-
- HY-32329
-
|
Setiptiline
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-13222
-
|
BAN ORL 24
|
Opioid Receptor
|
Cancer
Neurological Disease
|
|
BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.
|
-
- HY-B1448A
-
|
Benidipine
KW-3049 free base
|
Apoptosis
Calcium Channel
|
Cardiovascular Disease
|
|
Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
|
-
- HY-105201
-
|
Fabesetron
FK1052 free base
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
|
-
- HY-148350
-
|
DS69910557
|
Thyroid Hormone Receptor
|
Cancer
|
|
DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM. DS69910557 can be used for the research of hyperparathyroidism, hypercalcemia of malignancy and osteoporosis.
|
-
- HY-B0569
-
|
Hexamethonium Bromide
|
nAChR
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.
|
-
- HY-17582S
-
-
- HY-112667
-
-
- HY-U00263
-
-
- HY-B0355
-
-
- HY-101527
-
|
20-HEDE
WIT 002
|
Others
|
Cancer
|
|
20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
|
-
- HY-10259
-
-
- HY-110110A
-
-
- HY-14423
-
-
- HY-A0033
-
-
- HY-B0500
-
-
- HY-B1108
-
-
- HY-147403S
-
-
- HY-U00212
-
-
- HY-101177
-
-
- HY-11103
-
-
- HY-14369
-
-
- HY-18611A
-
-
- HY-14770
-
-
- HY-107765
-
-
- HY-108324
-
-
- HY-50669
-
-
- HY-10259A
-
-
- HY-G0011
-
-
- HY-14130
-
-
- HY-N9404
-
-
- HY-N1378
-
-
- HY-14447
-
-
- HY-106499
-
-
- HY-136842
-
-
- HY-U00335
-
-
- HY-101164
-
-
- HY-U00289
-
-
- HY-18611
-
-
- HY-19670
-
-
- HY-101683
-
-
- HY-14129
-
-
- HY-19855
-
-
- HY-15853
-
-
- HY-14367
-
-
- HY-145353
-
-
- HY-15640
-
-
- HY-13004
-
-
- HY-U00257
-
-
- HY-13796
-
-
- HY-103533
-
-
- HY-14432
-
-
- HY-101407
-
-
- HY-14263
-
|
Pericyazine
Propericiazine; RP 8909
|
Dopamine Receptor
|
Neurological Disease
|
|
Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.
|
-
- HY-B0781
-
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-103200
-
-
- HY-100672
-
-
- HY-114452
-
|
LY2940094
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
|
-
- HY-15129
-
|
O-Phospho-L-serine
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
|
-
- HY-116637
-
|
Tetrahydromagnolol
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
|
-
- HY-116216
-
|
PD 168368
|
Bombesin Receptor
|
Cancer
|
|
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.
|
-
- HY-103360
-
|
J-113863
|
CCR
|
Inflammation/Immunology
|
|
J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.
|
-
- HY-32329A
-
|
Setiptiline maleate
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
|
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-112558
-
-
- HY-N0184
-
-
- HY-P0171
-
-
- HY-50669A
-
-
- HY-15412
-
|
HhAntag
|
Smo
|
Cancer
|
|
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
|
-
- HY-16502
-
|
Transcrocetinate disodium
Disodium trans-crocetinate
|
iGluR
|
Cancer
|
|
Transcrocetinate disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-14538S
-
-
- HY-135552
-
-
- HY-10560
-
-
- HY-U00253
-
-
- HY-B1589AS
-
-
- HY-U00106
-
-
- HY-19632
-
-
- HY-19193
-
-
- HY-100152
-
-
- HY-134992
-
-
- HY-110136A
-
-
- HY-19391
-
-
- HY-16027
-
-
- HY-42937
-
|
Transcrocetin meglumine salt
trans-Crocetin meglumine salt
|
iGluR
|
Cancer
|
|
Transcrocetin meglumine salt, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-10052
-
-
- HY-U00252
-
-
- HY-105198
-
-
- HY-B0412
-
-
- HY-12752A
-
-
- HY-43711
-
-
- HY-B1510
-
-
- HY-17001A
-
-
- HY-19654
-
-
- HY-109511
-
|
AZD-1678
|
CCR
|
Others
|
|
AZD-1678 is a potent CCR4 receptor antagonist, with a pIC50 of 8.6.
|
-
- HY-101620
-
-
- HY-101700
-
-
- HY-101669
-
-
- HY-17505
-
-
- HY-101718
-
-
- HY-107631
-
-
- HY-103495
-
-
- HY-B0547
-
-
- HY-110136
-
-
- HY-14538S1
-
-
- HY-108997
-
-
- HY-108563
-
-
- HY-U00360
-
-
- HY-B1613A
-
-
- HY-15319B
-
-
- HY-100703
-
-
- HY-141487
-
-
- HY-16978
-
-
- HY-B1517A
-
|
Alprenolol hydrochloride
(RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride
|
5-HT Receptor
|
Cancer
|
|
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
|
-
- HY-B0561S1
-
-
- HY-B0561S
-
-
- HY-A0295
-
-
- HY-B1517
-
|
Alprenolol
(RS)-Alprenolol; dl-Alprenolol
|
5-HT Receptor
|
Cancer
|
|
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
|
-
- HY-G0014S
-
|
Quetiapine Sulfoxide-d8
|
Drug Metabolite
|
Neurological Disease
|
|
Quetiapine Sulfoxide-d8 (Quetiapine S-oxide-d8) is the deuterium labeled Quetiapine sulfoxide. Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.
|
-
- HY-B0774
-
-
- HY-B0538A
-
-
- HY-100318
-
-
- HY-105221
-
-
- HY-A0012
-
-
- HY-17512
-
-
- HY-15195
-
-
- HY-105771
-
-
- HY-W018061
-
-
- HY-20167A
-
-
- HY-12426A
-
-
- HY-13059B
-
-
- HY-U00356
-
-
- HY-15462
-
-
- HY-U00392
-
-
- HY-109167
-
-
- HY-19057A
-
-
- HY-B1435
-
-
- HY-142214
-
-
- HY-12426
-
-
- HY-13059
-
-
- HY-B0716
-
-
- HY-15411
-
-
- HY-107749
-
-
- HY-10634
-
-
- HY-107672
-
-
- HY-U00251
-
-
- HY-12799
-
-
- HY-103408
-
-
- HY-15835
-
|
CUDC-427
GDC-0917
|
IAP
|
Cancer
|
|
CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
|
-
- HY-U00084
-
-
- HY-19909
-
|
NRC-2694
|
EGFR
|
Cancer
|
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-19110
-
-
- HY-19274
-
-
- HY-B0547A
-
-
- HY-111398
-
-
- HY-U00105
-
-
- HY-15541
-
-
- HY-12377
-
-
- HY-10064
-
-
- HY-109718
-
-
- HY-125879
-
-
- HY-139567
-
-
- HY-142658
-
-
- HY-100308
-
-
- HY-14561A
-
|
Idazoxan hydrochloride
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
|
-
- HY-115487
-
|
MF-766
|
Prostaglandin Receptor
|
Cancer
Inflammation/Immunology
|
|
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research.
|
-
- HY-101755
-
-
- HY-14147
-
|
Renzapride
BRL 24924
|
5-HT Receptor
|
Metabolic Disease
|
|
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.
|
-
- HY-15403
-
-
- HY-103113
-
-
- HY-103407A
-
-
- HY-142617
-
-
- HY-10664
-
-
- HY-139572
-
-
- HY-13636B
-
|
Fulvestrant (R enantiomer)
ICI 182780 (R enantiomer); ZD 9238 (R enantiomer); ZM 182780 (R enantiomer)
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant R enantiomer (ICI 182780 R enantiomer) is the R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-13059A
-
-
- HY-120689
-
-
- HY-P2285
-
-
- HY-B0478
-
-
- HY-10995
-
-
- HY-19347
-
-
- HY-P1014
-
-
- HY-13534
-
-
- HY-76511
-
-
- HY-108688
-
-
- HY-A0021
-
-
- HY-16756
-
-
- HY-100882
-
-
- HY-A0018
-
-
- HY-120090
-
-
- HY-B0205S1
-
-
- HY-104061
-
-
- HY-101105A
-
-
- HY-10486
-
-
- HY-103189
-
-
- HY-104062
-
-
- HY-109841
-
-
- HY-B0780
-
-
- HY-105018
-
|
Epelsiban
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-B1438S1
-
-
- HY-17024
-
-
- HY-12428
-
-
- HY-123607
-
-
- HY-19191
-
-
- HY-12131
-
-
- HY-14938
-
-
- HY-19025
-
-
- HY-112710
-
-
- HY-118678
-
-
- HY-13636A
-
|
Fulvestrant (S enantiomer)
ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant S enantiomer (ICI 182780 S enantiomer) is the S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-U00143
-
-
- HY-P1572
-
-
- HY-N0145
-
-
- HY-12777
-
-
- HY-U00354
-
-
- HY-12301
-
-
- HY-N2332A
-
-
- HY-12715
-
-
- HY-B1164S
-
-
- HY-114452A
-
|
LY2940094 tartrate
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
|
-
- HY-B0781S
-
-
- HY-103197
-
|
2-Methoxyidazoxan monohydrochloride
RX821002 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2).
|
-
- HY-15084
-
-
- HY-111069
-
-
- HY-107679
-
-
- HY-12339
-
|
NVS-CRF38
|
CRFR
|
Endocrinology
|
|
NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
|
-
- HY-P1017
-
-
- HY-15009
-
-
- HY-111442
-
-
- HY-B0205S2
-
-
- HY-108251
-
-
- HY-137448
-
-
- HY-128351
-
-
- HY-U00433
-
-
- HY-19512
-
-
- HY-100717
-
-
- HY-145590
-
|
Retezorogant
|
ROR
|
Cancer
|
|
Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1.
|
-
- HY-19433A
-
-
- HY-15577
-
|
GSK3787
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-108626
-
|
ML154
NCGC84
|
Others
|
Neurological Disease
|
|
ML154 is a potent antagonist of NPSR. ML154 has the potential for the research of anxiety, addiction and food disorders.
|
-
- HY-132827
-
-
- HY-16168AS
-
-
- HY-12635
-
-
- HY-A0024
-
|
Tolterodine
(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
|
mAChR
|
Neurological Disease
|
|
Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-15068
-
|
NBQX
FG9202
|
iGluR
|
Neurological Disease
|
|
NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
|
-
- HY-103363
-
-
- HY-19736
-
-
- HY-19654B
-
-
- HY-B1059
-
-
- HY-B0595
-
-
- HY-W040146
-
-
- HY-102095
-
-
- HY-15403A
-
-
- HY-120546
-
-
- HY-136678A
-
-
- HY-115877
-
|
GDC-0334
|
TRP Channel
|
Others
|
|
GDC-0334 is a TRPA1 antagonist useful in treatment TRPA1-mediated diseases, such as pain or asthma.
|
-
- HY-12380A
-
-
- HY-A0252
-
-
- HY-A0163
-
-
- HY-103126
-
-
- HY-B0205S
-
-
- HY-118180
-
-
- HY-114745
-
|
MoTP
|
Others
|
Cancer
|
|
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
|
-
- HY-112895
-
|
UT-155
|
Androgen Receptor
|
Cancer
|
|
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
|
-
- HY-U00402
-
-
- HY-101259
-
-
- HY-19097
-
-
- HY-U00077
-
-
- HY-19048
-
-
- HY-19499
-
-
- HY-U00028
-
-
- HY-U00237
-
-
- HY-B1305
-
-
- HY-101022
-
-
- HY-P0061A
-
-
- HY-14467
-
-
- HY-A0125A
-
-
- HY-19733
-
|
Lumateperone tosylate
ITI-007 tosylate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
|
-
- HY-17637
-
|
Lumateperone
ITI-007
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
|
-
- HY-P1309A
-
-
- HY-103104
-
|
Fananserin
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
|
-
- HY-124290
-
|
Carotegrast methyl
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-32329S
-
|
Setiptiline-d3
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-14249
-
-
- HY-109077S
-
-
- HY-15538
-
-
- HY-N4247
-
-
- HY-107616
-
|
H2L5186303
|
LPL Receptor
|
Others
|
|
H2L5186303 is a potent and selective LPA 2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM.
|
-
- HY-135363
-
-
- HY-18287
-
|
MRT-83
|
Smo
|
Cancer
|
|
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
|
-
- HY-101139A
-
-
- HY-101986
-
-
- HY-101486
-
|
LF3
|
β-catenin
|
Cancer
|
|
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
|
-
- HY-101586
-
-
- HY-12506A
-
|
Naspm trihydrochloride
1-Naphthylacetyl spermine trihydrochloride
|
iGluR
|
Neurological Disease
|
|
Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
|
-
- HY-109565
-
|
ASTX660
|
IAP
Apoptosis
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-A0178
-
-
- HY-16985
-
|
Darolutamide
ODM-201; BAY-1841788
|
Androgen Receptor
|
Cancer
|
|
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
|
-
- HY-100985
-
-
- HY-12488
-
-
- HY-15726
-
-
- HY-122974
-
-
- HY-14284S
-
-
- HY-B0686
-
-
- HY-15851
-
-
- HY-12940
-
-
- HY-12380
-
-
- HY-P0009B
-
-
- HY-N0382
-
|
Galangin
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-18966
-
-
- HY-P0009A
-
-
- HY-U00137
-
-
- HY-104020A
-
-
- HY-16060
-
-
- HY-110255
-
-
- HY-18204
-
-
- HY-P1726
-
-
- HY-101395
-
-
- HY-A0013A
-
-
- HY-13534A
-
-
- HY-101720
-
|
Fradafiban
BIBU-52
|
Integrin
|
Cardiovascular Disease
|
|
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-101598
-
-
- HY-15105
-
-
- HY-101686
-
-
- HY-15853A
-
-
- HY-107699
-
-
- HY-A0013
-
-
- HY-110255A
-
-
- HY-10888
-
-
- HY-15481
-
-
- HY-103153
-
-
- HY-100407
-
|
JNJ16259685
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-P3671
-
-
- HY-14542A
-
-
- HY-18263C
-
|
Elubrixin tosylate
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
|
-
- HY-14542C
-
-
- HY-18263A
-
|
Elubrixin
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
|
-
- HY-14263S
-
|
Pericyazine-d4
|
Dopamine Receptor
|
Neurological Disease
|
|
Pericyazine-d4 (Propericiazine-d4) is the deuterium labeled Pericyazine. Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.
|
-
- HY-17407
-
-
- HY-B1510S
-
