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Results for "

modulators

" in MCE Product Catalog:

806

Inhibitors & Agonists

13

Screening Libraries

1

Dye Reagents

3

Biochemical Assay Reagents

37

Peptides

2

Inhibitory Antibodies

63

Natural
Products

60

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-103715
    NLRP3 modulators 1

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107).
  • HY-50900
    gamma-Secretase Modulators

    Amyloid-β production inhibitor; γ-Secretase modulators

    Amyloid-β Neurological Disease
    gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor.
  • HY-145300
    nAChR modulator-2

    nAChR Infection
    nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator.
  • HY-145299
    nAChR modulator-1

    nAChR Infection
    nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator.
  • HY-141692B
    (R)-IL-17 modulator 4

    Interleukin Related Inflammation/Immunology
    (R)-IL-17 modulator 4 is the R-configure of IL-17 modulator 4 (HY-141692). IL-17 modulator 4 is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.
  • HY-142030
    TRPC5 modulator-1

    TRP Channel Neurological Disease
    TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of <1 nM for the research of neuropsychiatry disorders.
  • HY-147530
    mGluR2 modulator 4

    mGluR Neurological Disease
    mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic.
  • HY-147528
    mGluR2 modulator 2

    mGluR Neurological Disease
    mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic.
  • HY-146117
    P-gp modulator 2

    P-glycoprotein Cancer
    P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
  • HY-146118
    P-gp modulator 3

    P-glycoprotein Cancer
    P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
  • HY-142940
    RORγt modulator 5

    ROR Inflammation/Immunology
    RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2).
  • HY-145429
    IL-17A modulator-2

    Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    IL-17A modulator-2 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 27. IL-17A modulator-2 inhibits the biological action of IL-17A with a pIC50 of 8.3. IL-17A modulator-2 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders.
  • HY-115923
    Nur77 modulator 2

    Others Inflammation/Immunology
    Nur77 modulator 2, a Nur77 modulator (Kd of 0.35 μM), is a potent and orally active inflammation inhibitor. Nur77 modulator 2 modulates the colocalization of Nur77 at mitochondria.
  • HY-146151
    γ-Secretase modulator 12

    γ-secretase Amyloid-β Neurological Disease
    γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice.
  • HY-145430
    IL-17A modulator-1

    Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders.
  • HY-109152
    Navocaftor

    GLPG 3067; ABBV-3067

    CFTR Others
    Navocaftor (GLPG 3067), as a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, example 1).
  • HY-144373
    IL-17 modulator 6

    Interleukin Related Inflammation/Immunology
    IL-17 modulator 6 (compound 61) is a potent Interleukin 17 (IL-17) modulator (pIC50=9.1). IL-17 modulator 6 has the ability to inhibit IL-17 and can be used for the treatment of inflammatory and autoimmune diseases.
  • HY-114863
    PHCCC(4Me)

    THCCC

    mGluR Neurological Disease
    PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator.
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • HY-101058
    PD1-PDL1-IN 1

    PD-1/PD-L1 Inflammation/Immunology
    PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator.
  • HY-108572
    S26948

    PPAR Metabolic Disease Cardiovascular Disease
    S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ.
  • HY-103475
    GS39783

    GABA Receptor Neurological Disease
    GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction.
  • HY-110191
    VU0469650

    mGluR Cancer Neurological Disease
    VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM.
  • HY-142723
    KCa2 channel modulator 1

    Potassium Channel Neurological Disease
    KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype.
  • HY-116855
    TASP0433864

    mGluR Neurological Disease
    TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.
  • HY-144320
    HBV-IN-17

    HBV Infection
    HBV-IN-17 (compound 8) is a potent HBV capsid assembly modulator with an EC50 of 511 nM.
  • HY-142735
    KCa2 channel modulator 2

    Potassium Channel Neurological Disease
    KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively
  • HY-120023
    VU0453595

    mAChR Neurological Disease
    VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia.
  • HY-13017S
    Ivacaftor-d9

    VX-770-d9

    CFTR Cancer
    Ivacaftor-D9 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research.
  • HY-130630
    mGluR2 modulator 1

    mGluR Neurological Disease
    mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research.
  • HY-113689
    GAT211

    Cannabinoid Receptor Neurological Disease
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 can be used for neuropathic and/or inflammatory pain research.
  • HY-145871
    BA38017

    HBV Infection
    BA38017 is a potent HBV core protein assembly modulator. BA38017 inhibits HBV replication with an EC50 of 0.20 μM.
  • HY-107682
    TQS

    nAChR Inflammation/Immunology Neurological Disease
    TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.
  • HY-100605
    VU0483605

    mGluR Others
    VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively.
  • HY-122025
    AC-262536

    Androgen Receptor Metabolic Disease
    AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM).
  • HY-117861
    ML198

    Glucosidase Metabolic Disease
    ML198 is a glucocerebrosidase (GCase) modulator with an EC50 of 0.4 μM. ML198 is an activator and non-inhibitory chaperone of glucocerebrosidase. ML198 can be used for the research of Gaucher disease.
  • HY-10933
    CX516

    BDP 12

    iGluR Neurological Disease
    CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
  • HY-143312
    V-0219

    GCGR Metabolic Disease
    V-0219 (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 can be used for obesity-associated diabetes research.
  • HY-144291
    LY3154885

    Dopamine Receptor Neurological Disease
    LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved drug-drug interactions (DDI) risk profile.
  • HY-145585
    Onfasprodil

    iGluR Neurological Disease
    Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A).
  • HY-12567
    ML375

    VU0483253

    mAChR Neurological Disease
    ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4.
  • HY-117959
    TAK-615

    LPL Receptor Inflammation/Immunology
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
  • HY-W074890
    Palmitoylglycine

    N-palmitoyl glycine

    Calcium Channel NO Synthase Inflammation/Immunology Neurological Disease
    Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide (NO) production in sensory neurons.
  • HY-114348
    N,N'-Diacetyl-L-cystine

    DiNAC; (Ac-Cys-OH)2

    Others Cardiovascular Disease
    N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-139091
    FEMA 4774

    Others Others
    FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer.
  • HY-103561
    DCB

    mGluR Neurological Disease
    DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).
  • HY-142936
    RORγt modulator 3

    ROR Inflammation/Immunology Cancer Neurological Disease
    RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
  • HY-N2509
    Iristectorigenin B

    Iristectrigenin B

    LXR Cardiovascular Disease
    Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β.
  • HY-17609
    Difelikefalin

    CR-845; FE-202845

    Opioid Receptor Neurological Disease
    Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
  • HY-142935
    RORγt modulator 2

    ROR Inflammation/Immunology Cancer Neurological Disease
    RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
  • HY-124600
    NVR 3-778

    HBV Infection
    NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
  • HY-101165
    Cyclothiazide

    iGluR Neurological Disease
    Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current.
  • HY-118301
    ADX71441

    GABA Receptor Neurological Disease
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.
  • HY-121736
    AGI-12026

    AGI-026

    Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma.
  • HY-A0106
    (S)-(-)-Levamisole

    Levamisole; L-Tetramisole; Levamisol

    nAChR Infection Inflammation/Immunology
    (S)-(-)-Levamisole (Levamisole), an anthelmintic agent with immunomodulatory properties. (S)-(-)-Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active.
  • HY-117734
    PYD-106

    iGluR Neurological Disease
    PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors.
  • HY-12439
    ML380

    mAChR Neurological Disease
    ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
  • HY-120576
    ML169

    VU0405652

    mAChR Neurological Disease
    ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease.
  • HY-117851
    AC-265347

    CaSR Metabolic Disease Endocrinology
    AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases.
  • HY-113008A
    cis-Urocanic acid

    (Z)-Urocanic acid; cis-UCA

    5-HT Receptor Inflammation/Immunology
    cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-144698
    mGlu4 receptor agonist 1

    mGluR Neurological Disease
    mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect.
  • HY-A0037
    Lasofoxifene

    CP-336156

    Estrogen Receptor/ERR Cancer Inflammation/Immunology
    Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.
  • HY-100979
    W-84 dibromide

    HDMPPA

    mAChR Others
    W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine.
  • HY-13757AS
    Tamoxifen-​d5

    ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-144705
    GAT564

    Cannabinoid Receptor Neurological Disease
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.
  • HY-120645
    BMS-986122

    Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes.
  • HY-147149
    BPN-15477

    Others Neurological Disease
    BPN-15477 is a potent SMC (splicing modulator compound) that restores correct splicing of ELP1 (Elongator complex protein 1) exon 20. BPN-15477 corrects splicing of the ELP1 transcript, significantly increases the level of functional protein in vivo in all tissues, including brain. BPN-15477 can be used for frontotemporal dementia research.
  • HY-147681
    SUN13837

    FGFR Neurological Disease
    SUN13837 is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. SUN13837 shows neuroprotective activity. SUN13837 can be used for neurodegenerative diseases research.
  • HY-101422
    GAL-021

    Potassium Channel Inflammation/Immunology
    GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates.
  • HY-A0038
    Lasofoxifene tartrate

    CP-336156 tartrate

    Estrogen Receptor/ERR Endocrinology Cancer
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-drug like properties and clinical candidate potential. .
  • HY-139897
    CX 717

    iGluR Neurological Disease
    CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD).
  • HY-101422A
    GAL-021 sulfate

    Potassium Channel Inflammation/Immunology
    GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates.
  • HY-103520
    DS2

    GABA Receptor Neurological Disease
    DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
  • HY-A0036
    Bazedoxifene acetate

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-147683
    FGFR-IN-3

    FGFR Neurological Disease
    FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research.
  • HY-114978
    VU0424465

    mGluR PERK Neurological Disease
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.
  • HY-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-A0031A
    Bazedoxifene hydrochloride

    TSE-424 hydrochloride

    Estrogen Receptor/ERR Cancer
    Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
  • HY-111052
    AZD7325

    GABA Receptor Cytochrome P450 Inflammation/Immunology Neurological Disease
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
  • HY-141899
    MK-6884

    mAChR Neurological Disease
    MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent.
  • HY-124803
    GPCR modulator-1

    GCGR Metabolic Disease
    GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research.
  • HY-144501
    D18

    Toll-like Receptor (TLR) PD-1/PD-L1 Cancer Inflammation/Immunology
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2.
  • HY-147684
    FGFR-IN-7

    FGFR Neurological Disease
    FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research.
  • HY-135671
    AhR modulator-1

    Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR Cancer Endocrinology
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
  • HY-141692
    IL-17 modulator 4

    Interleukin Related Inflammation/Immunology
    IL-17 modulator 4 is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.
  • HY-B0300
    Penicillamine

    D-(-)-Penicillamine

    Drug Metabolite Inflammation/Immunology Cancer
    Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine increases free copper and enhances oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-141692A
    IL-17 modulator 4 sulfate

    Interleukin Related Inflammation/Immunology
    IL-17 modulator 4 sulfate is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.
  • HY-146053
    CXCR4 modulator-1

    CXCR Cancer Infection Inflammation/Immunology
    CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV.
  • HY-10018
    Toll-like receptor modulator

    Toll-like Receptor (TLR) Inflammation/Immunology
    Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
  • HY-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • HY-107506
    Ro 67-4853

    mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.
  • HY-145759
    Mutant p53 modulator-1

    MDM-2/p53 Cancer
    Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B).
  • HY-147657
    GABAA receptor modulator-2

    GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
  • HY-147105
    LRH-1 modulator-1

    Others Inflammation/Immunology
    LRH-1 modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1 modulator-1 shows anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 induces anti-inflammatory cytokine IL-10, and reduces inflammatory cytokine IL-1b and TNFa.
  • HY-128334
    PCSK9 modulator-2

    Others Metabolic Disease
    PCSK9 modulator-2 (Compound 1) is a potent modulator of PCSK9 with an EC50 value of 202 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-2 has the potential for the research of hyperlipidemia.
  • HY-15618
    MK-7622

    M1 receptor modulator

    mAChR Neurological Disease
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
  • HY-145370
    GluN2B receptor modulator-1

    iGluR Neurological Disease
    GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
  • HY-146084
    PCSK9 modulator-3

    Others Metabolic Disease
    PCSK9 modulator-3 (Compound 13) is a potent modulator of PCSK9 with an EC50 value of 2.46 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-3 has the potential for the research of hyperlipidemia.
  • HY-146085
    PCSK9 modulator-4

    Others Metabolic Disease
    PCSK9 modulator-4 (Compound 21) is a potent modulator of PCSK9 with an EC50 value of 0.15 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-4 has the potential for the research of hyperlipidemia.
  • HY-147228
    NR2F6 modulator-1

    Others Cancer Inflammation/Immunology
    NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity.
  • HY-142939
    RORγt modulator 4

    ROR Cancer Inflammation/Immunology
    RORγt modulator 4 is a RORγt modulator. RORγt modulator 4 has an activity to modulate IL-17A production in cells derived from mouse spleen (WO2018030550A1; compound 146).
  • HY-116553
    FzM1

    Wnt β-catenin Cancer
    FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade.
  • HY-50889
    gamma-secretase modulator 3

    γ-secretase Neurological Disease
    gamma-secretase modulator 3 is a gamma-secretase modulator.
  • HY-143390
    NMDA receptor modulator 2

    iGluR Neurological Disease
    NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research.
  • HY-141832
    mGluR5 modulator 1

    mGluR Neurological Disease
    mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments.
  • HY-143396
    NMDA receptor modulator 5

    iGluR Neurological Disease
    NMDA receptor modulator 5 (Compound 195) is a potent NMDA receptor modulator. NMDA receptor modulator 5 can be used for neurological disorder research.
  • HY-143393
    NMDA receptor modulator 4

    iGluR Neurological Disease
    NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research.
  • HY-143391
    NMDA receptor modulator 3

    iGluR Neurological Disease
    NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator. NMDA receptor modulator 3 can be used for neurological disorder research.
  • HY-143397
    NMDA receptor modulator 6

    iGluR Neurological Disease
    NMDA receptor modulator 6 (Compound 183) is a potent NMDA receptor modulator. NMDA receptor modulator 6 can be used for neurological disorder research.
  • HY-145997
    MRGPRX4 modulator-1

    Others Inflammation/Immunology
    MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders.
  • HY-146054
    CXCR4 modulator-2

    CXCR Inflammation/Immunology
    CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model.
  • HY-147051
    MRGPRX4 modulator-2

    Others Inflammation/Immunology
    MRGPRX4 modulator-2 (compound 1-55) is a potent MRGPR X4 modulator, possessing antagonist activity against MRGPR X4 with an IC50 < 100 nM. MRGPRX4 modulator-2 can be used for researching autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson’s Syndrome, and other chronic itch conditions.
  • HY-145372
    γ-Secretase modulator 10

    γ-secretase Neurological Disease
    γ-Secretase modulator 10 is a novel γ-secretase modulator.
  • HY-109168
    Bersacapavir

    JNJ-6379; JNJ-56136379

    HBV Infection
    Bersacapavir is a novel Hepatitis B Virus capsid assembly modulator.
  • HY-135419
    CB2 modulator 1

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia.
  • HY-N6905
    Acetylarenobufagin

    HIF/HIF Prolyl-Hydroxylase Cancer
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
  • HY-138040
    CRBN modulator-1

    Ligands for E3 Ligase Cancer
    CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
  • HY-139203
    IL-17 modulator 3

    Interleukin Related Cancer Inflammation/Immunology
    IL-17 modulator 3 is an IL-17 modulator (US20200247785A1). IL-17 modulator 3 can be used for the research of inflammation, cancer and autoimmune diseases.
  • HY-136275
    AMPA receptor modulator-2

    iGluR Others
    AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor. pIC50 = -lgIC50.
  • HY-50754
    gamma-secretase modulator 2

    γ-secretase Neurological Disease
    gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.
  • HY-147720A
    γ-Secretase modulator 11 hydrochloride

    γ-secretase Neurological Disease
    γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease.
  • HY-111996
    Kv3 modulator 1

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.
  • HY-112154
    CXCR7 modulator 2

    CXCR Cardiovascular Disease Endocrinology
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-U00135
    Calcium channel-modulator-1

    Calcium Channel Cardiovascular Disease
    Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC50 of 0.8 μM.
  • HY-147260
    Dalzanemdor

    SAGE-718

    iGluR Others
    Dalzanemdor (SAGE-718) is a N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator.
  • HY-147234
    Sirtuin modulator 2

    Sirtuin Cancer Metabolic Disease Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Sirtuin modulator 2 (Compound 132) is a sirtuin modulator with an ED50 equal or less than 50 μM.
  • HY-110201
    Estrogen receptor modulator 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
  • HY-146152
    ASGPR modulator-1

    Others Others
    ASGPR modulator-1 (Compound 5TJX) is a macrocycle compound that can be uesd for protein-protein interaction study.
  • HY-U00429
    NOT Receptor Modulator 1

    Others Neurological Disease
    NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
  • HY-U00420
    Opioid receptor modulator 1

    Opioid Receptor Neurological Disease
    Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
  • HY-107987
    CXCR7 modulator 1

    CXCR Endocrinology
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  • HY-147559
    CB1R Allosteric modulator 2

    Cannabinoid Receptor Others
    CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
  • HY-147558
    CB1R Allosteric modulator 1

    Cannabinoid Receptor Others
    CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
  • HY-147529
    mGluR2 modulator 3

    mGluR Neurological Disease
    mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
  • HY-147757
    PPARγ/δ modulator 1

    PPAR Metabolic Disease
    PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively.
  • HY-144399
    CD33 splicing modulator 1

    Others Neurological Disease
    CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 has the potential for the research of neurodegenerative disease including Alzheimer's disease.
  • HY-141535A
    IL-17 modulator 1 disodium

    Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-50162
    GPR120 modulator 1

    Free Fatty Acid Receptor Metabolic Disease
    GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-112699
    AMPA receptor modulator-1

    iGluR Neurological Disease
    AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
  • HY-50172
    GPR120 modulator 2

    Free Fatty Acid Receptor Metabolic Disease
    GPR120 modulator 2 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F13. GPR120 modulator 2 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-124906
    JAMI1001A

    iGluR Neurological Disease
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
  • HY-141535
    IL-17 modulator 1

    Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, treating or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
  • HY-16734A
    Amiselimod hydrochloride

    MT-1303 hydrochloride

    LPL Receptor Cancer
    Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
  • HY-19758A
    Sirtuin modulator 1

    Sirtuin Cancer
    Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
  • HY-105272A
    Loreclezole hydrochloride

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-105272
    Loreclezole

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-145872
    HBV-IN-20

    HBV Infection
    HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators).
  • HY-108714
    NGP555

    γ-secretase Neurological Disease
    NGP555 is a γ-secretase modulator.
  • HY-111763
    GPR40/FFAR1 modulator 1

    Free Fatty Acid Receptor Metabolic Disease
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  • HY-110122
    AZ 12216052

    mGluR Others
    AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.
  • HY-128831
    Kv3 modulator 4

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.
  • HY-114314
    BA-53038B

    HBV Infection
    BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-139740
    Aβ Fibrillization modulator 1

    Amyloid-β Neurological Disease
    Aβ Fibrillization modulator 1 stabilizes monomers.
  • HY-112819
    Insulin levels modulator

    Insulin Receptor Metabolic Disease Endocrinology
    Insulin levels modulator could be used to treat diabetes.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-16563
    Narciclasine

    Lycoricidinol

    ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
  • HY-141840
    GLP-1R modulator C5

    GCGR Metabolic Disease
    GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).
  • HY-136651
    BNTA

    Others Inflammation/Immunology
    BNTA, a potent extracellular matrix (ECM) modulator, facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA shows a promising potential for osteoarthritis alleviation by modulating cartilage generation.
  • HY-141839
    GLP-1R modulator C16

    GCGR Metabolic Disease
    GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
  • HY-128581
    γ-Secretase modulator 4

    γ-secretase Neurological Disease
    γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively.
  • HY-19487
    Ribocil

    Bacterial Infection
    Ribocil is a highly selective chemical modulator of bacterial riboflavin riboswitches.
  • HY-103668A
    SSD114 hydrochloride

    GABA Receptor Neurological Disease
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
  • HY-139556
    Zavacorilant

    Glucocorticoid Receptor Metabolic Disease
    Zavacorilant is capable of modulating glucocorticoid receptor (GR).
  • HY-B0463
    Clomiphene citrate

    Clomifene citrate

    Estrogen Receptor/ERR Endocrinology
    Clomiphene citrate (Clomifene citrate) is a selective estrogen receptor modulator.
  • HY-13047
    S-(+)-Mecamylamine hydrochloride

    Dexmecamylamine hydrochloride; TC-5214 hydrochloride

    nAChR Neurological Disease
    S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.
  • HY-101216
    Org-26576

    iGluR Neurological Disease
    Org-26576 is a AMPA receptor positive allosteric modulator.
  • HY-101858
    BQCA

    mAChR Neurological Disease
    BQCA a highly selective allosteric modulator of the M1 mAChR.
  • HY-128829
    Kv3 modulator 2

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
  • HY-141842
    GLP-1R modulator L7-028

    GCGR Metabolic Disease
    GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM).
  • HY-111386
    E-7386

    Epigenetic Reader Domain Cancer
    E-7386 is an orally active CBP/beta-catenin modulator.
  • HY-114530
    LY2452473

    Androgen Receptor Cancer Metabolic Disease
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-N0273
    Brassinolide

    Brassin lactone

    Apoptosis Cancer
    Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
  • HY-100186
    GSK-2881078

    Androgen Receptor Neurological Disease
    GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia.
  • HY-18705
    Azoramide

    Apoptosis Endocrinology
    Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
  • HY-101845
    FITM

    mGluR Cancer
    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  • HY-107457
    AZD-8529

    mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-100550
    MSDC 0160

    Mitoglitazone; CAY10415

    Insulin Receptor Mitochondrial Metabolism Neurological Disease Endocrinology
    MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
  • HY-147560
    σ1 Receptor/μ Opioid receptor modulator 1

    Sigma Receptor Opioid Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain.
  • HY-P3455
    Ac-SVVVRT-NH2

    PGC-1α Cancer Metabolic Disease
    Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α.
  • HY-136621
    5-HT1A modulator 2 hydrochloride

    5-HT Receptor Neurological Disease
    5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT (HY-112061), is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding.
  • HY-100507
    Avadomide

    CC 122

    E1/E2/E3 Enzyme Apoptosis Cancer Inflammation/Immunology
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-106182
    TBC3711

    Endothelin Receptor Endocrinology
    TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
  • HY-16716
    Basmisanil

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-107507
    Ro 01-6128

    mGluR Neurological Disease
    Ro 01-6128 is a positive allosteric modulator of mGluR1.
  • HY-101488
    CC-885

    Ligands for E3 Ligase Cancer
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
  • HY-B1405
    Dehydroisoandrosterone 3-acetate

    Dehydroepiandrosterone 3-acetate; DHEA acetate

    Androgen Receptor Endocrinology Cancer
    Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
  • HY-112788
    ONO-8590580

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • HY-107457A
    AZD-8529 mesylate

    mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-107661
    Arundic Acid

    ONO-2506; (R)-2-Propyloctanoic acid

    Others Neurological Disease
    Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
  • HY-12812
    Autotaxin modulator 1

    Phosphodiesterase (PDE) Cancer Neurological Disease
    Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.
  • HY-145343
    RO7185876

    γ-secretase Neurological Disease
    RO7185876 is a potent and selective gamma secretase modulator as a potential treatment for Alzheimer's disease.
  • HY-111453
    Velsecorat

    AZD7594; AZ13189620

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
  • HY-112564
    JNJ-632

    HBV Infection
    JNJ-632 is a hepatitis B virus (HBV) capsid assembly modulator (CAM).
  • HY-143225
    NCGC00538431

    Others Others
    NCGC00538431 is a potent modulator of SIRPα-CD47.
  • HY-145603
    Vanzacaftor

    CFTR Inflammation/Immunology
    Vanzacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR) for treating cystic fibrosis.
  • HY-U00178
    Idoxifene

    CB7432

    Estrogen Receptor/ERR Cancer
    Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
  • HY-117291A
    XMD-17-51 Trifluoroacetate

    Others Others
    XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that is able to modulate protein kinases.
  • HY-N2371
    27-Hydroxycholesterol

    Estrogen Receptor/ERR LXR Endogenous Metabolite Cancer
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-15476
    VU 0364439

    mGluR Neurological Disease
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
  • HY-U00339
    H3 receptor-MO-1

    Histamine Receptor Endocrinology
    H3 receptor-MO-1 is a modulator of histamine H3 receptor.
  • HY-146468
    DPP-4/GPR119 modulator 1

    Dipeptidyl Peptidase GPR119 Potassium Channel Metabolic Disease
    DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 µM. DPP-4/GPR119 modulator 1 can be used for diabetes research.
  • HY-146677
    5-HT6R/MAO-B modulator 1

    5-HT Receptor Monoamine Oxidase Neurological Disease
    5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits.
  • HY-138690
    Estrogen receptor modulator 6

    Estrogen Receptor/ERR Endocrinology
    Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM).
  • HY-10937
    Farampator

    CX-691; Org24448

    iGluR Neurological Disease
    Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.
  • HY-109073
    Rovazolac

    LXR Inflammation/Immunology
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
  • HY-19559
    JNJ-46778212

    VU 0409551

    mGluR Neurological Disease
    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  • HY-107651
    VU 0365114

    mAChR Others
    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
  • HY-124670
    1beta-Hydroxyalantolactone

    Others Inflammation/Immunology
    1beta-Hydroxyalantolactone modulate many processes that influence inflammatory reactions.
  • HY-114775
    RCGD423

    Interleukin Related Inflammation/Immunology Neurological Disease
    RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
  • HY-143435
    AG6033

    Apoptosis Others Cancer
    AG6033 is a potential novel CRBN modulator. AG6033 suppresses various tumor cells by modulating the interactions between CRBN and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces CRBN-dependent cytotoxic effect.
  • HY-16940
    24(S)-Hydroxycholesterol

    24S-OHC; 24S-HC; Cerebrosterol

    LXR iGluR Endogenous Metabolite Metabolic Disease
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
  • HY-139583
    Sunobinop

    S 117957; IMB 115

    Opioid Receptor Neurological Disease
    Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1).
  • HY-115726
    FRM-024

    γ-secretase Neurological Disease
    FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.
  • HY-P0079
    Neuromedin N

    Neuromedin N (rat, mouse, porcine, canine)

    Dopamine Receptor Neurological Disease
    Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes.
  • HY-18102A
    GLPG0492 (R enantiomer)

    Androgen Receptor Neurological Disease
    GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.
  • HY-13724B
    Pipendoxifene hydrochloride

    Estrogen Receptor/ERR Cancer
    Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
  • HY-13058B
    (R)-ADX-47273

    mGluR Neurological Disease
    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  • HY-121848
    VU0155094

    ML397

    mGluR Neurological Disease
    VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.
  • HY-13262
    Lumacaftor

    VX-809; VRT 826809

    CFTR Autophagy Inflammation/Immunology
    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • HY-Y0248A
    Farnesol

    Endogenous Metabolite Bacterial Antibiotic Infection Cancer
    Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
  • HY-11027
    MK-0773

    PF-05314882

    Androgen Receptor Endocrinology
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
  • HY-10932
    Aniracetam

    Ro 13-5057

    nAChR iGluR Neurological Disease
    Aniracetam(Ro 13-5057) is a nootropics and neuroprotective drug, which is selectively modulates the AMPA receptor and nAChR.
  • HY-125120
    Kansuiphorin C

    Others Others
    Kansuiphorin C ameliorates malignant ascites by modulating gut microbiota and related metabolic functions.
  • HY-139715
    IMD-ferulic

    NF-κB Cancer
    IMD-ferulic is a covalently linked NF-κB modulator that improves the adjuvanticity of small molecule immune potentiators.
  • HY-128830
    Kv3 modulator 3

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
  • HY-134130
    Integrin modulator 1

    Integrin Inflammation/Immunology
    Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
  • HY-18162
    JNJ-42153605

    mGluR Neurological Disease
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
  • HY-19720
    Emixustat

    ACU-4429

    Others Metabolic Disease
    Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
  • HY-16998
    SR2211

    ROR Inflammation/Immunology
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
  • HY-131364
    Nur77 modulator 1

    Others Cancer
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
  • HY-139044
    VU6000918

    mAChR Neurological Disease
    VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.
  • HY-16766
    Decoglurant

    RO4995819

    mGluR Neurological Disease
    Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-18292
    ARN2966

    Amyloid-β Neurological Disease
    ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
  • HY-100728
    BMT-145027

    mGluR Neurological Disease
    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  • HY-144322
    HBV-IN-18

    HBV Infection
    HBV-IN-18 (Compound 3) is an HBV capsid assembly modulator (CpAM) with an EC50 of 2790 nM.
  • HY-100298
    Caldaret

    MCC-135

    Na+/Ca2+ Exchanger Cardiovascular Disease
    Caldaret is an intracellular Ca 2+ handling modulator that acts through reverse mode Na +/Ca 2+ exchanger inhibition.
  • HY-109046
    Tulrampator

    CX-1632

    iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • HY-103573
    VU 0360223

    mGluR Neurological Disease
    VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM.
  • HY-115879
    SHR168442

    ROR Cancer Inflammation/Immunology
    SHR168442 is a modulator of retinoid-related orphan receptor gamma (RORγ) with an IC50 value of 0.035 μM.
  • HY-111498
    RGX-104 hydrochloride

    LXR Cancer Inflammation/Immunology
    RGX-104 hydrochloride is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-B1390B
    Saccharin sodium hydrate

    Bacterial Inflammation/Immunology
    Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties.
  • HY-119810
    Seletracetam

    Ucb 44212

    Others Neurological Disease
    Seletracetam (Ucb 44212), as an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy.
  • HY-112267
    Olacaftor

    VX-440

    CFTR Autophagy Inflammation/Immunology
    Olacaftor (VX-440) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator extracted from patent US9782408.
  • HY-145434
    IL-17 modulator 5

    Interleukin Related Inflammation/Immunology
    IL-17 modulator 5 (compound 26) is a IL-17 inhibitor, with an IC50 of 1 nM.
  • HY-111536
    Mitochonic acid 5

    MA-5

    Mitochondrial Metabolism Cardiovascular Disease
    Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
  • HY-17590
    Radafaxine hydrochloride

    GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
  • HY-17030
    Acamprosate calcium

    Calcium N-acetylhomotaurinate

    GABA Receptor Neurological Disease
    Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
  • HY-125880
    SBI-553

    Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-112282
    BI-1408

    γ-secretase Neurological Disease
    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for 42.
  • HY-16423
    Rapacuronium bromide

    Org 9487

    mAChR Neurological Disease
    Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  • HY-14419
    TCN238

    mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • HY-Y0272
    Saccharin

    Bacterial Inflammation/Immunology
    Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
  • HY-121577
    Sonlicromanol

    KH176

    Reactive Oxygen Species Metabolic Disease
    Sonlicromanol (KH176) is an orally active reactive oxygen species (ROS) modulator for the study in mitochondrial disease.
  • HY-B2121
    6-Methoxy-2-naphthoic acid

    Naproxen impurity O

    iGluR Neurological Disease
    6-Methoxy-2-naphthoic acid is an NMDA receptor modulator extracted from patent WO 2012019106 A2.
  • HY-112633
    SMN-C3

    DNA/RNA Synthesis Others
    SMN-C3 is an orally active SMN2 splicing modulator and has the potential to treat spinal muscular atrophy (SMA).
  • HY-16728
    Rapastinel

    GLYX-13

    iGluR Neurological Disease
    Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
  • HY-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-107218
    11-Hydroxysugiol

    RAR/RXR VD/VDR Infection
    11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).
  • HY-103498
    Org20599

    GABA Receptor Neurological Disease
    Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.
  • HY-124419
    RO0711401

    mGluR Neurological Disease
    RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.
  • HY-113346
    Tetrahydrodeoxycorticosterone

    Tetrahydro-11-deoxycorticosterone

    GABA Receptor Neurological Disease
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
  • HY-107456
    E6130

    CX3CR1 Inflammation/Immunology Endocrinology
    E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
  • HY-120024
    BMS-986188

    Opioid Receptor Neurological Disease
    BMS-986188 is a selective positive allosteric modulator of δ-opioid receptor with an EC50 of 0.05 μM.
  • HY-119941
    VU0652835

    mGluR Neurological Disease
    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  • HY-19872
    AZD-6280

    GABA Receptor Neurological Disease
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
  • HY-101583
    NEO 376

    SPI-376

    5-HT Receptor GABA Receptor Dopamine Receptor Neurological Disease
    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  • HY-13574A
    Biricodar

    VX-710

    P-glycoprotein Cancer
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  • HY-119810A
    Seletracetam lithium

    Ucb 44212 lithium

    HIV Neurological Disease
    Seletracetam (Ucb 44212) lithium, as an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy.
  • HY-124958
    NDMC101

    NF-κB Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-146469
    DPP-4/GPR119 modulator 2

    Dipeptidyl Peptidase GPR119 Metabolic Disease
    DPP-4/GPR119 modulator 2 (Compound 20i) is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist with an IC50 of 0.22 µM for DPP-IV and an EC50 of 0.95 µM for GPR119. DPP-4/GPR119 modulator 2 can be used for diabetes research.
  • HY-147556
    SK3 Channel-IN-1

    Potassium Channel Cancer
    SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer.
  • HY-128799A
    CL097 hydrochloride

    Toll-like Receptor (TLR) Reactive Oxygen Species Inflammation/Immunology
    CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
  • HY-128799
    CL097

    Toll-like Receptor (TLR) Reactive Oxygen Species Inflammation/Immunology
    CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
  • HY-130680
    Syk-IN-3

    Syk Cancer
    Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
  • HY-118424
    JNJ-55511118

    iGluR Neurological Disease
    JNJ-55511118 is a highly potent, reversible, and selective AMPA receptor inhibitor selective for TARP-γ8. JNJ-55511118 fully displaces the radioligand (20 nM) with the Ki of 26 nM in competition binding experiments. JNJ-55511118 is a tool molecule with potential therapeutic utility as an anticonvulsant or neuroprotectant.
  • HY-W001692
    Ocinaplon

    DOV 273547

    GABA Receptor Neurological Disease
    Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit.
  • HY-100084
    Methyl-3β-hydroxycholenate

    ROR Inflammation/Immunology
    Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
  • HY-139742
    ADTL-SA1215

    Sirtuin Cancer
    ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
  • HY-139574
    Firzacorvir

    HBV Infection Inflammation/Immunology
    Firzacorvir is a cyclic sulfamide compound and modulates HBV core protein. Firzacorvir has anti-HBV activity with EC50 < 1 μΜ.
  • HY-15204
    Tonabersat

    SB-220453

    Gap Junction Protein Inflammation/Immunology Neurological Disease
    Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system.
  • HY-16950B
    (E)-4-Hydroxytamoxifen

    (E)-Afimoxifene

    Estrogen Receptor/ERR Cancer
    (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
  • HY-18654
    ADX88178

    mGluR Neurological Disease
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  • HY-119810B
    Seletracetam lithium bromide

    Ucb 44212 lithium bromide

    Others Neurological Disease
    Seletracetam (Ucb 44212) lithium bromide, an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy.
  • HY-109037
    Mavacamten

    MYK461; SAR439152

    Myosin Cardiovascular Disease
    Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
  • HY-P1562
    PUMA BH3

    Bcl-2 Family Cancer
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-142162
    LSN3318839

    GCGR Metabolic Disease
    LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).
  • HY-12157
    VU 0238429

    mAChR Others
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
  • HY-U00013
    Nitroflurbiprofen

    HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen

    COX Cardiovascular Disease
    Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
  • HY-101746
    GSK376501A

    PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  • HY-112920
    TM-25659

    Others Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
  • HY-119687
    Bifenazate

    GABA Receptor Infection
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor.
  • HY-13288
    Org 27569

    Cannabinoid Receptor Neurological Disease
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
  • HY-111098
    GSK1702934A

    TRP Channel Cardiovascular Disease
    GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
  • HY-10043
    gamma-secretase modulator 1

    γ-secretase Neurological Disease
    γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-12509
    PEPA

    iGluR Neurological Disease
    PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
  • HY-17030S
    Acamprosate D3 calcium

    GABA Receptor Neurological Disease
    Acamprosate D3 calcium is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems.
  • HY-137204
    COR659

    GABA Receptor Neurological Disease
    COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.
  • HY-119078
    VU0080241

    mGluR Neurological Disease
    VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM.
  • HY-15748
    JNJ-40411813

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
  • HY-100366
    Lu AF21934

    mGluR Neurological Disease
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
  • HY-129086
    BPAM344

    iGluR Neurological Disease
    BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM).
  • HY-U00366
    S1PR1-MO-1

    LPL Receptor Inflammation/Immunology
    S1PR-MO-1 is the modulator of sphingosine-1-phosphate receptor, used for research of hyperproliferative, inflammatory diseases.
  • HY-112426
    LAU159

    GABA Receptor Neurological Disease
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  • HY-16728B
    Rapastinel Trifluoroacetate

    GLYX-13 Trifluoroacetate

    iGluR Neurological Disease
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-B1494
    Picrotoxinin

    Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors.
  • HY-122138
    VU6010572

    mGluR Neurological Disease
    VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant.
  • HY-146979
    hA2A/hCA XII modulator 1

    Adenosine Receptor Carbonic Anhydrase Cancer
    hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.
  • HY-114269
    (-)-(S)-B-973B

    nAChR Neurological Disease
    (-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.
  • HY-145413
    BRD2889

    Gutathione S-transferase Cancer
    BRD2889 is an analog of the alkaloid piperlongumine. BRD2889 is a robust modulator of the GSTP1-ISCU axis in pulmonary hypertension (PH).
  • HY-19371
    Lorediplon

    GABA Receptor Neurological Disease
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
  • HY-103035
    BIO-32546

    Phosphodiesterase (PDE) Cancer
    BIO-32546 (example 12b, S-isomer) is an autotaxin (ATX) modulator, extracted from the patent US20170158687A1.
  • HY-16951
    VU-1545

    mGluR Neurological Disease
    VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM.
  • HY-112814
    VU6001376

    mGluR Neurological Disease
    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  • HY-111246
    MK-3984

    Androgen Receptor Cancer
    MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer.
  • HY-131658
    VEGFR-2-IN-6

    VEGFR Others
    VEGFR-2-IN-6 (example 64) is a VEGFR2 inhibitor (angiogenesis modulator), which is extracted from patent WO 02/059110.
  • HY-U00151
    Dopropidil

    Calcium Channel Cardiovascular Disease
    Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.
  • HY-112781
    Pesampator

    PF-04958242

    iGluR Neurological Disease
    Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM.
  • HY-116896
    LY117018

    Estrogen Receptor/ERR Cancer
    LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
  • HY-100409
    PHCCC

    mGluR Cancer
    PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
  • HY-N0299
    Stachyose hydrate

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Stachyose hydrate act as a prebiotic to enhance the growth and activity of beneficial bacteria. Stachyose hydrate exhibit a hypoglycemic effect, and improve inflammation through modulating gut microbiota.
  • HY-Y0248AS
    Farnesol-d6

    Endogenous Metabolite Bacterial Antibiotic Infection Cancer
    Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
  • HY-132806
    Alogabat

    GABA Receptor Neurological Disease
    Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1).
  • HY-W014102
    L-Alanyl-L-glutamine

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations.
  • HY-12505
    CX546

    iGluR Autophagy Neurological Disease
    CX546 is a first-generation and selective benzamide-type positive AMPAR modulator. CX546 is a prototypical ampakine agent and has antipsychotic effects.
  • HY-143715
    Cereblon inhibitor 1

    Ligands for E3 Ligase Cancer
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research.
  • HY-107661A
    S-(+)-Arundic Acid

    (S)ONO-2506; (S)-2-Propyloctanoic acid

    Others Others
    S-(+)-Arundic Acid ((S)ONO-2506) is the S-enantiomer of Arundic Acid. Arundic acid is an astrocyte-modulating agent, has the potential for stroke and Alzheimer’s disease research.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-120274
    AZD9977

    Mineralocorticoid Receptor Metabolic Disease Cardiovascular Disease
    AZD9977 is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. AZD9977 is used for heart failure, and chronic kidney disease research.
  • HY-N2487
    5-Hydroxy-7-acetoxyflavone

    Others Cancer
    5-Hydroxy-7-acetoxyflavone, an active natural flavone derivative found in various plant sources, modulates several biological activities.
  • HY-119433
    Asoprisnil

    J867

    Progesterone Receptor Endocrinology
    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  • HY-125265
    JTP-117968

    Glucocorticoid Receptor Metabolic Disease
    JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC50 of 6.8 nM), exhibits improved transrepression/transactivation dissociation.
  • HY-U00068
    PPARα-MO-1

    PPAR Metabolic Disease
    PPARα-MO-1 is a potent PPARα modulator extracted from patent WO/2004/110982A1, formula I.
  • HY-13277
    IRAK inhibitor 3

    IRAK Inflammation/Immunology
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  • HY-W010452
    3-Hydroxybutyric acid sodium

    β-Hydroxybutyric acid sodium

    Endogenous Metabolite Metabolic Disease
    3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids.
  • HY-10043A
    gamma-secretase modulator 1 hydrochloride

    γ-secretase Neurological Disease
    gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-N2370
    24-Hydroxycholesterol

    iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
  • HY-113378
    3-Hydroxybutyric acid

    β-Hydroxybutyric acid

    Endogenous Metabolite Metabolic Disease
    3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids.
  • HY-111498A
    RGX-104

    LXR Cancer Inflammation/Immunology
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-124622
    NNC-0640

    GCGR Metabolic Disease
    NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM.
  • HY-116463
    E1R

    Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
  • HY-N3755
    Dihydroresveratrol

    Estrogen Receptor/ERR Cancer
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
  • HY-14758
    Adipiplon

    NG2-73

    GABA Receptor Neurological Disease
    Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.
  • HY-B1221S
    Flufenamic acid-d4

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-144635
    Nrf2-ARE/hMAO-B/QR2 modulator 1

    Monoamine Oxidase Keap1-Nrf2 ROS Kinase Neurological Disease
    Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC50s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices.
  • HY-14425
    NB001

    HTS 09836

    Adenylate Cyclase Neurological Disease
    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  • HY-10937S
    Farampator-d10

    iGluR Neurological Disease
    Farampator-d10 (CX-691-d10) is the deuterium labeled Farampator. Farampator (CX-691) is an AMPA receptor positive modulator.
  • HY-129946
    Dopamine D2 receptor antagonist-1

    Dopamine Receptor Neurological Disease
    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.
  • HY-101363
    1-BCP

    Piperonylic acid piperidide

    iGluR Neurological Disease
    1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
  • HY-120722
    TCH-165

    Proteasome Cancer
    TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
  • HY-133555
    mGluR2 antagonist 1

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
  • HY-P1562A
    PUMA BH3 TFA

    Bcl-2 Family Cancer
    PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-101855
    Anle138b

    Amyloid-β Neurological Disease
    Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
  • HY-147705
    PPARγ phosphorylation inhibitor 1

    PPAR Metabolic Disease
    PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.
  • HY-123396
    8-Chloro-cAMP

    PKA Cancer
    8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity.
  • HY-18102
    GLPG0492

    Androgen Receptor Others
    GLPG0492 is a non-steroidal selective androgen receptor modulator (potency 12 nM). GLPG0492 has the potential for the research of musculo-skeletal diseases such as sarcopenia and cachexia.
  • HY-132812
    Emraclidine

    CVL-231

    mAChR Neurological Disease
    Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.
  • HY-Y0272S
    Saccharin-d4

    Bacterial Inflammation/Immunology
    Saccharin-d4 is the deuterium labeled Saccharin. Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
  • HY-14399
    Itanapraced

    CHF5074; CSP-1103

    γ-secretase Neurological Disease
    Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
  • HY-123837
    MLS1082

    Dopamine Receptor Neurological Disease
    MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling.
  • HY-12212
    Omaveloxolone

    RTA 408

    Keap1-Nrf2 STING Apoptosis Cancer Inflammation/Immunology
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
  • HY-120332
    Sonlicromanol hydrochloride

    KH176 hydrochloride

    Reactive Oxygen Species Metabolic Disease
    Sonlicromanol (KH176) hydrochloride, a chemical entity derivative of Trolox, is a blood-brain barrier permeable ROS-redox modulator. Sonlicromanol (KH176) hydrochloride is used in the study for mitochondrial disorders.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-138937
    NDB

    FXR Metabolic Disease
    NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.
  • HY-14774S
    (Rac)-Monepantel-d5

    nAChR Cancer
    (Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-N0549
    (-)-α-Pinene

    GABA Receptor Bacterial Virus Protease Endogenous Metabolite Neurological Disease
    (-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
  • HY-B1221S1
    Flufenamic acid-13C6

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-132811
    Dazucorilant

    CORT113176

    Glucocorticoid Receptor Inflammation/Immunology Neurological Disease
    Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders.
  • HY-N2096
    Kavain

    GABA Receptor Neurological Disease
    Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
  • HY-144319
    SHR5133

    HBV Infection
    SHR5133 is a highly potent, orally active HBV capsid assembly modulator. SHR5133 displays HBV DNA reduction (EC50=26.6 nM).
  • HY-13556A
    Arzoxifene hydrochloride

    LY353381 hydrochloride; SERM III hydrochloride

    Estrogen Receptor/ERR Cancer
    Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
  • HY-14774S1
    (Rac)-Monepantel sulfone-d5

    nAChR Cancer
    (Rac)-Monepantel sulfone-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-139580
    Plazinemdor

    iGluR Neurological Disease
    Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system..
  • HY-143212
    18:0-22:6 DG

    1-Stearoyl-2-docosahexaenoyl-sn-glycerol

    p38 MAPK Others
    18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol that can bind to RasGRP and modulate MAP kinases activation.
  • HY-137986
    LUF7244

    Potassium Channel Inflammation/Immunology
    LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research.
  • HY-119165
    GSM-1

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
  • HY-120797
    CRT0273750

    Others Cancer
    CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
  • HY-N3308
    Medicarpin

    Apoptosis Cancer
    Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs.
  • HY-114406
    TD-106

    Ligands for E3 Ligase Cancer
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
  • HY-107409
    GNE 5729

    iGluR Neurological Disease
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
  • HY-121095
    Bizine

    Histone Demethylase Cancer Neurological Disease
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects.
  • HY-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-103306
    Ryanodine

    Others Neurological Disease
    Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
  • HY-14383
    Vosilasarm

    RAD140

    Androgen Receptor Endocrinology Neurological Disease
    Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors.
  • HY-N4157
    Isopteropodine

    mAChR 5-HT Receptor Neurological Disease
    Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors.
  • HY-113346S
    Tetrahydrodeoxycorticosterone-d3

    Tetrahydro-11-deoxycorticosterone-d3

    GABA Receptor Endogenous Metabolite
    Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
  • HY-109187
    Posenacaftor

    PTI-801

    CFTR Inflammation/Immunology
    Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF).
  • HY-P1125
    4-CMTB

    Free Fatty Acid Receptor Others
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
  • HY-W010104
    L-Methionine sulfoxide

    H-Met(O)-OH

    Endogenous Metabolite Metabolic Disease
    L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.
  • HY-110190
    VU0422288

    ML396

    mGluR Neurological Disease
    VU0422288 is a positive allosteric modulator of group III mGluRs with EC50 values of 108, 146, and 128 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays.
  • HY-128400
    4'-Methoxychalcone

    PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  • HY-109187A
    Posenacaftor sodium

    PTI-801 sodium

    CFTR Inflammation/Immunology
    Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).
  • HY-107498
    GNE-8324

    iGluR Neurological Disease
    GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons.
  • HY-14959
    Ulipristal

    CDB-3236; Deacetyl CDB-2914

    Progesterone Receptor Cancer Endocrinology
    Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
  • HY-15393
    VU 0357121

    mGluR Neurological Disease
    VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-12288
    Ozanimod

    RPC-1063

    LPL Receptor Inflammation/Immunology Neurological Disease
    Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod (RPC-1063) has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod (RPC-1063) can be used for the research of relapsing multiple sclerosis (MS) .
  • HY-131941
    SJM-3

    GABA Receptor Neurological Disease
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.
  • HY-16636
    ML337

    mGluR Neurological Disease
    ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile.
  • HY-112256
    ACP-105

    Androgen Receptor Inflammation/Immunology
    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 hydrochloride

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-110278
    ADX71743

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
  • HY-129395
    Mezigdomide

    CC-92480

    E1/E2/E3 Enzyme Molecular Glues Apoptosis Cancer
    Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating drug (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity.
  • HY-128128
    ASN04421891

    Others Neurological Disease
    ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
  • HY-131181
    LEI-401

    Phospholipase Neurological Disease
    LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.
  • HY-108250
    (R)-Bicalutamide

    Androgen Receptor Cancer
    (R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
  • HY-122751
    (R)-DNMDP

    Phosphodiesterase (PDE) Cancer
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line.
  • HY-19845A
    Piperidine-MO-1

    Dopamine Receptor Neurological Disease
    Piperidine-MO-1 is a modulator of dopamine receptor extracted from patent WO/2005/121087A1, compound example 2; exhibits an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.
  • HY-21290
    SU-4942

    Tyrosinase Cancer
    SU-4942 is a tyrosine kinase signal signal modulator. SU-4942 inhibits VEGF- and endothelial cell growth factor (ECGF)-induced mitogenesis in endothelial cells (US5792783A).
  • HY-128770
    LY3154207

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
  • HY-120530
    JNJ-46281222

    mGluR Neurological Disease
    JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
  • HY-108337
    GNE-0723

    iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
  • HY-125740
    Malvidin-3-glucoside chloride

    Malvidin-3-O-glucoside chloride; Oenin chloride

    Others Inflammation/Immunology
    Malvidin-3-glucoside chloride (Malvidin-3-O-glucoside chloride), a major wine anthocyanin, is effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation.
  • HY-108703
    Foliglurax

    PXT002331

    mGluR Neurological Disease
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-108243
    AZD5423

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
  • HY-107902
    RIG-1 modulator 1

    HBV HCV HIV Influenza Virus Infection
    RIG-1 modulator 1 is an anti-viral compound which can be useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV extracted from patent WO 2015172099 A1.
  • HY-147315
    CFTR corrector 9

    CFTR Others
    CFTR corrector 9 (compound 42) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator. CFTR corrector 9 can be used for researching cystic fibrosis (CF) and other CFTR associated disorders.
  • HY-143226
    DK1

    Estrogen Receptor/ERR Metabolic Disease
    DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRα receptor. DK1 has the potential for the research of diabetes.
  • HY-105858
    BNC210

    H-Ile-Trp-OH; IW-2143

    nAChR Neurological Disease
    BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
  • HY-12151
    NS 1738

    NSC 213859

    nAChR Neurological Disease
    NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
  • HY-13738A
    Raloxifene hydrochloride

    Keoxifene hydrochloride; LY156758; LY139481 hydrochloride

    Estrogen Receptor/ERR Autophagy Endocrinology Cancer
    Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
  • HY-N2585
    Isodeoxyelephantopin

    Reactive Oxygen Species NF-κB Autophagy Cancer
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
  • HY-14859
    Dipraglurant

    ADX48621

    mGluR Neurological Disease
    Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.
  • HY-129527
    GNE-9278

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    GABA Receptor Neurological Disease
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • 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-W011509
    CyPPA

    Potassium Channel Neurological Disease
    CyPPA is a positive modulator of hSK3 and hSK2, with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels[1]
  • HY-139784
    Idroxioleic acid

    (R)-2-Hydroxyoleic acid; (R)-2-OHOA

    Others Cancer
    Idroxioleic acid ((R)-2-Hydroxyoleic acid; (R)-2-OHOA), the R enantiomer of (Rac)-Idroxioleic acid, is an orally active fatty acid that modulates the lipid composition and structure of the membranes. Idroxioleic acid has antitumor activities.
  • 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-108710
    VU0650786

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-106406
    Benzylacyclouridine

    BAU; 5-Benzylacyclouridine

    Others Cancer
    Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives.
  • HY-108703A
    Foliglurax monohydrochloride

    PXT002331 (monohydrochloride)

    mGluR Neurological Disease
    Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-12324
    SB269652

    Dopamine Receptor Neurological Disease
    SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  • HY-113920A
    Azumolene

    EU4093 free base

    Calcium Channel Metabolic Disease
    Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
  • HY-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-12795
    Vps34-IN-1

    PI3K Autophagy Cancer
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
  • HY-16950A
    (E/Z)-4-Hydroxytamoxifen

    Afimoxifene

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen receptor modulator.
  • HY-101792A
    RG7800 hydrochloride

    RO6885247 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.
  • 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-134194
    KL201

    Others Metabolic Disease
    KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues.
  • HY-144734
    Pantothenate kinase-IN-1

    Others Neurological Disease
    Pantothenate kinase-IN-1 (Compound 1) is a pantothenate kinase (PANK) modulator with an IC50 of 0.51 µM against PANK3. Pantothenate kinase-IN-1 has a reasonable ligand efficiency (LipE = 2.8).
  • HY-124867
    D3-βArr

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  • HY-105296
    Blarcamesine

    Sigma Receptor mAChR
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
  • HY-13738
    Raloxifene

    Keoxifene; LY156758 free base; LY139481

    Estrogen Receptor/ERR Cancer
    Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-B1837
    Cyfluthrin

    Sodium Channel Infection
    Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
  • HY-134661
    (S)-CVN424

    Others Neurological Disease
    (S)-CVN424 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. (S)-CVN424 has the potential for a variety of neurological and psychiatric disorders research, including Parkinson's disease.
  • HY-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
  • HY-P1397
    RVD-Hpα

    Cannabinoid Receptor Neurological Disease
    RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2.
  • HY-13963
    ZCL278

    Ras Cancer
    ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
  • HY-119332
    3-Keto petromyzonol

    Others Endocrinology
    3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey.
  • HY-120012
    AZD9567

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
  • HY-107091
    Aspartyl-alanyl-diketopiperazine

    DA-DKP

    Others Inflammation/Immunology
    Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
  • HY-14417
    VU0155041

    mGluR Neurological Disease
    VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
  • HY-122190
    TAK-071

    mAChR Neurological Disease
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  • HY-16508
    Ulipristal acetate

    CDB-2914

    Progesterone Receptor Autophagy Endocrinology Cancer
    Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
  • HY-15731
    Estetrol

    Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
  • HY-112209
    VU0467154

    mAChR Neurological Disease
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-101281
    VU 6008667

    mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
  • HY-116273
    ML299

    Phospholipase Cancer
    ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells.
  • HY-W011100
    Cyclofenil

    Estrogen Receptor/ERR Influenza Virus Infection Endocrinology
    Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
  • HY-B0723
    Ospemifene

    FC-1271a

    Estrogen Receptor/ERR Cancer
    Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
  • HY-12508
    CMPDA

    iGluR Neurological Disease
    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
  • HY-109187B
    (R)-Posenacaftor sodium

    (R)-PTI-801 sodium

    CFTR Inflammation/Immunology
    (R)-Posenacaftor (R)-PTI-801) sodium is the R enantiomer of Posenacaftor. Posenacaftor is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF).
  • HY-107198
    (2S)-6-Prenylnaringenin

    GABA Receptor Neurological Disease
    (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.
  • HY-14417B
    VU0155041 sodium

    mGluR Neurological Disease
    VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
  • HY-111772
    Elexacaftor

    VX-445

    CFTR Autophagy Others
    Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
  • HY-145601
    Tinengotinib

    Aurora Kinase VEGFR Cancer
    Tinengotinib is the modulator of one or more protein kinases such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential for the research of these kinase abnormalities diseases mediated, especially cancer-related diseases (extracted from patent WO2018108079A1).
  • HY-B0282
    Acetylcholine chloride

    ACh chloride

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.
  • HY-N2409
    Delphinidin chloride

    Apoptosis JAK STAT Cancer Cardiovascular Disease
    Delphinidin chloride, an anthocyanidin, is isolated from berries and red wine. Delphinidin chloride shows endothelium-dependent vasorelaxation. Delphinidin chloride also can modulate JAK/STAT3 and MAPKinase signaling to induce apoptosis in HCT116 cells.
  • HY-13058
    ADX-47273

    mGluR Neurological Disease
    ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
  • HY-N4180
    Pennogenin 3-O-beta-chacotrioside

    Autophagy Cancer
    Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
  • HY-135585
    LY88074

    Others Endocrinology
    LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
  • HY-141515
    BMS-986121

    Opioid Receptor Neurological Disease
    BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.
  • HY-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-B2158
    Chlorotrianisene

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-123268
    Ro 363

    Adrenergic Receptor Cardiovascular Disease
    Ro 363, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. RO 363 is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
  • HY-123268A
    Ro 363 hydrochloride

    Adrenergic Receptor Cardiovascular Disease
    Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
  • HY-136151
    UNC10217938A

    Others Others
    UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
  • HY-50856S
    Deuruxolitinib

    CTP-543; Ruxolitinib D8; Deuterated Ruxolitinib

    JAK Inflammation/Immunology
    Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).
  • HY-116819
    VU0453379

    GCGR Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-120589
    VU0360172

    mGluR Neurological Disease
    VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice.
  • HY-101291
    Iberdomide

    CC-220

    Ligands for E3 Ligase Apoptosis Inflammation/Immunology Cancer
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
  • HY-131004
    CB2R PAM

    Cannabinoid Receptor Neurological Disease
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.
  • HY-103572
    MNI137

    mGluR Neurological Disease
    MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.
  • HY-134377
    Bocidelpar

    PPAR Metabolic Disease
    Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b).
  • HY-135572
    TLX agonist 1

    Others Cancer Neurological Disease
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.
  • HY-109160
    Rimtuzalcap

    CAD-1883

    Potassium Channel Neurological Disease
    Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA).
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-B0005A
    Toremifene

    Z-Toremifene; NK 622 free base; FC-1157a free base

    Estrogen Receptor/ERR Cancer Infection
    Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
  • HY-146099
    GABAA receptor agent 7

    GABA Receptor Neurological Disease
    GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy.
  • HY-110180
    VU0409106

    mGluR Neurological Disease
    VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
  • HY-144377
    RXR antagonist 1

    RAR/RXR Cancer Metabolic Disease Neurological Disease
    RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research.
  • HY-128677
    NCC007

    Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-108523
    LG100754

    UVI 2112

    RAR/RXR Metabolic Disease
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
  • HY-146100
    GABAA receptor agent 8

    GABA Receptor Neurological Disease
    GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.
  • HY-101528
    IDRA 21

    iGluR Neurological Disease
    IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging.
  • HY-146391
    P-gp inhibitor 4

    P-glycoprotein Cancer
    P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
  • 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-B0106
    Levetiracetam

    UCB L059

    DNA Methyltransferase Cancer Neurological Disease
    Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent.
  • HY-103040
    Zuranolone

    GABA Receptor Neurological Disease
    Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-N0029
    Forsythoside B

    TNF Receptor NF-κB Inflammation/Immunology
    Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
  • HY-100290
    5-HT1A modulator 1

    5-HT Receptor Neurological Disease
    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  • HY-107734
    L 152804

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  • HY-N0513
    Loganic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
  • HY-121149
    Droloxifene

    3-Hydroxytamoxifen

    Estrogen Receptor/ERR Apoptosis Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
  • HY-125096
    C108297

    Glucocorticoid Receptor Metabolic Disease Inflammation/Immunology
    C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation.
  • HY-14569
    CDPPB

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
  • HY-14612
    CPPHA

    mGluR Neurological Disease
    CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.
  • HY-122515
    Fulvic Acid

    Others Metabolic Disease Inflammation/Immunology
    Fulvic Acid is a natural product, which comes from humic substances produced by microorganisms in soil. Fulvic Acid can modulate the immune system, influence the oxidative state of cells, and improve gastrointestinal function. Fulvic Acid has the potential for researching chronic inflammatory diseases, including diabetes.
  • HY-N6694
    4-Bromo A23187

    Calcium Channel Bacterial Apoptosis Antibiotic Cancer Infection
    4-Bromo A23187 is a halogenated analog of the highly selective calcium ionophore A-23187. 4-Bromo A23187,a calcium modulator, induces apoptosis in different cells, including HL-60 cells.
  • HY-130800
    Eragidomide

    CC-90009

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer Inflammation/Immunology
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation.
  • HY-P1222
    LL-37, human

    Bacterial Infection
    LL-37, human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, human could help protect the cornea from infection and modulates wound healing.
  • HY-122487
    Troriluzole

    BHV-4157

    Others Neurological Disease
    Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
  • HY-145931
    CC214-2

    mTOR Cancer
    CC214-2 is a potent and dual inhibitor of mTORC1/mTORC2. Mycobacterium tuberculosis modulates mammalian target of rapamycin (mTOR) signaling to impede autophagy. CC214-2 has the potential to shorten the duration of TB.
  • HY-113608
    VCP171

    Adenosine Receptor Neurological Disease
    VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.
  • HY-P1222B
    LL-37, human acetate

    Bacterial Infection Inflammation/Immunology
    LL-37, human acetate is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, human acetate could help protect the cornea from infection and modulates wound healing.
  • HY-115467
    MitoBloCK-10

    Others Metabolic Disease
    MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
  • HY-13556
    Arzoxifene

    LY353381; SERM III

    Estrogen Receptor/ERR Metabolic Disease
    Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
  • HY-114933
    VU0119498

    mAChR Metabolic Disease
    VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity.
  • HY-123956
    HG-12-6

    IRAK Inflammation/Immunology
    HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
  • HY-119433S
    Asoprisnil-d3

    J867-d3

    Progesterone Receptor Endocrinology
    Asoprisnil-d3 (J867-d3) is the deuterium labeled Asoprisnil. Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  • HY-12023
    GTx-007

    S-4

    Androgen Receptor Cancer
    GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.
  • 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-143321
    STING agonist-13

    STING Cancer
    STING agonist-13 is a stimulator of interferon genes (STING) agonist, for cancer immunity via STING-mediated immune activation. STING agonist-13 can stimulate STING downstream signaling and promoting type I interferon immune responses. STING agonist-13 significantly decreases tumor volume and shows immunological memory-derived cancer inhibition.
  • HY-124569
    NAB-14

    iGluR Neurological Disease
    NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-13738S
    Raloxifene-d4

    Estrogen Receptor/ERR Cancer
    Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-144782
    HDAC10-IN-2

    HDAC Autophagy Cancer
    HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.
  • HY-B1786A
    (E/Z)-Sulindac sulfide

    γ-secretase Amyloid-β Neurological Disease
    (E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease.
  • HY-146237
    CC-99282

    Ligands for E3 Ligase Cancer
    CC-99282 is a potent and orally active cereblon (CRBN) E3 ligase modulator (CELMoD). CC-99282 co-opts CRBN to induce potent and targeted degradation of Ikaros and Aiolos. CC-99282 can be used for researching non-Hodgkin lymphomas.
  • HY-16579
    Etifoxine hydrochloride

    HOE 36-801 hydrochloride

    GABA Receptor Neurological Disease
    Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-110152
    LSN2463359

    mGluR Neurological Disease
    LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model.
  • HY-143878
    MRGPRX1 agonist 2

    Others Neurological Disease
    MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain.
  • HY-B0005
    Toremifene citrate

    Z-Toremifene citrate; NK 622; FC-1157a

    Estrogen Receptor/ERR Apoptosis Cancer Infection
    Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
  • HY-113320S1
    Etiocholanolone-d2

    5β-Androsterone-d2

    GABA Receptor Endogenous Metabolite
    Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • HY-16579A
    Etifoxine

    HOE 36-801

    GABA Receptor Neurological Disease
    Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-144779
    HDAC10-IN-1

    HDAC Autophagy Cancer
    HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.
  • HY-13738S2
    Raloxifene-d4 hydrochloride

    Estrogen Receptor/ERR Cancer
    Raloxifene-d4 hydrochloride is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-13738S3
    Raloxifene-d10

    Estrogen Receptor/ERR Cancer
    Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-B0719
    Ingenol Mebutate

    Ingenol 3-angelate; PEP005

    PKC Cancer Inflammation/Immunology
    Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Cancer
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
  • HY-126145
    S1PR1 modulator 1

    LPL Receptor Inflammation/Immunology
    S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.
  • HY-110114
    Gue1654

    Others Others
    Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ.
  • HY-128584
    VU6005806

    AZN-00016130

    mAChR Neurological Disease
    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
  • HY-116463D
    (Rac)-E1R

    Sigma Receptor Neurological Disease
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
  • HY-111475
    Mitochondrial fusion promoter M1

    Mitochondrial Metabolism Cardiovascular Disease
    Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator. Mitochondrial fusion promoter M1 preserves the mitochondrial function and promotes cellular respiration. Mitochondrial fusion promoter M1 alleviates cardiac and brain damage in rats with cardiac ischemia/reperfusion injury.
  • 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-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-143879
    MRGPRX1 agonist 3

    Others Neurological Disease
    MRGPRX1 agonist 3 (compound 1f) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.22 μM. MRGPRX1 agonist 3 can be used for researching neuropathic pain.
  • HY-B0909
    Triflupromazine hydrochloride

    Dopamine Receptor 5-HT Receptor Bacterial Autophagy Infection Neurological Disease
    Triflupromazine hydrochloride is an antipsychotic agent. Triflupromazine hydrochloride is Dopamine D1/D2 receptor antagonist and serotonin receptor 5-HT2 modulator. Triflupromazine hydrochloride also exhibits significant antibacterial activity against Gram-positive and Gram-negative bacteria.
  • HY-15731S
    Estetrol-d4

    Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol-d4 is the deuterium labeled Estetrol. Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
  • HY-106901A
    Asoxime dichloride

    HI-6

    nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • HY-P1222A
    LL-37, human TFA

    Bacterial Infection
    LL-37, human TFA is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, human TFA could help protect the cornea from infection and modulates wound healing.
  • HY-12762
    QS11

    Others Cancer
    QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
  • HY-P3102
    GLP-1(32-36)amide

    GCGR Metabolic Disease
    GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.
  • HY-P2454
    CSP1

    Bacterial Infection
    CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.
  • HY-10933S
    CX516-d10

    BDP 12-d10

    iGluR Neurological Disease
    CX516-d10 (BDP 12-d10) is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
  • HY-16508S
    Ulipristal acetate-d6

    CDB-2914-d6

    Progesterone Receptor Autophagy Endocrinology Cancer
    Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
  • HY-B2158S
    Chlorotrianisene-d9

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • HY-16950BS
    (E)-4-Hydroxytamoxifen-d5

    (E)-Afimoxifene-d5

    Estrogen Receptor/ERR Cancer
    (E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
  • HY-114739
    MA-0204

    PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-13738S1
    Raloxifene-d4 Bismethyl Ether

    Estrogen Receptor/ERR Cancer
    Raloxifene-d4 Bismethyl Ether is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-13580S
    Budesonide-d8

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide-d8 is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-103502
    CGP7930

    GABA Receptor Neurological Disease
    CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons.
  • HY-14611
    3,3'-Difluorobenzaldazine

    DFB

    mGluR Neurological Disease
    3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range.
  • HY-16950
    4-Hydroxytamoxifen

    (Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene

    Estrogen Receptor/ERR Cancer
    4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation.
  • HY-120613
    BMS-986187

    Opioid Receptor Neurological Disease
    BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM).
  • HY-P1303
    CART(62-76)(human,rat)

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • 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-110113
    CTA056

    Btk Cancer
    CTA056 is an ITK (IL-2-inducible T-cell kinase) inhibitor with an IC50 of 0.1 μM. CTA056 selectively targets malignant T cells and modulates oncomirs. CTA056 induces apoptosis and is a potential therapeutic agent for the treatment of T-cell leukemia and lymphoma.
  • HY-145559
    Cemdomespib

    KU-596

    HSP Metabolic Disease
    Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response.
  • HY-110168
    NS 9283

    nAChR Neurological Disease
    NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease.
  • HY-118342
    PQCA

    mAChR Neurological Disease
    PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
  • HY-118256
    LSN2814617

    mGluR Neurological Disease
    LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Cardiovascular Disease
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
  • HY-B0005AS
    Toremifene-d6

    Z-Toremifene-d6; NK 622-d6 free base; FC-1157a-d6 free base

    Estrogen Receptor/ERR Cancer Infection
    Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
  • HY-142941
    Glucocorticoid receptor-IN-1

    Glucocorticoid Receptor MMP Inflammation/Immunology
    Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV.
  • HY-N6084
    Humulone

    α-Lupulic acid

    COX GABA Receptor Apoptosis Cardiovascular Disease
    Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
  • HY-B1805
    Triclocarban

    3,4,4′-Trichlorocarbanilide

    Bacterial Infection
    Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes.
  • HY-113378S
    3-Hydroxybutyric acid-d4 sodium

    β-Hydroxybutyric acid-d4 sodium

    Endogenous Metabolite Metabolic Disease
    3-Hydroxybutyric acid-d4 (β-Hydroxybutyric acid-d4) sodium is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids.
  • HY-129811
    Bis-ANS dipotassium

    Microtubule/Tubulin Neurological Disease
    Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations.
  • HY-147158
    ZXH-1-161

    Ligands for E3 Ligase Cancer
    ZXH-1-161 is a potent cereblon (CRBN) modulator with an IC50 value of 39 nM in MM1.S wild type cells. ZXH-1-161 has selective degradation activity towards GSPT1. ZXH-1-161 can be used for researching multiple myeloma.
  • HY-124614
    GLP-26

    HBV Infection
    GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM. GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
  • HY-N6950
    Hederacolchiside A1

    PI3K Akt mTOR Parasite Apoptosis Cancer Infection
    Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
  • HY-101064
    Fmoc-leucine

    N-FMOC-leucine; NPC 15199; NSC 334290

    PPAR Metabolic Disease
    Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity.
  • HY-122579
    IGS-1.76

    Others Others
    IGS-1.76 efficiently inhibits the human NCS-1/Ric8a complex. IGS-1.76 shows a significantly increased affinity for hNCS-1 and is able to modulate the hNCS-1/Ric8a interaction efficiently.
  • HY-120727
    VU0364289

    mGluR Neurological Disease
    VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.
  • HY-P3102A
    GLP-1(32-36)amide TFA

    GCGR Metabolic Disease
    GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.
  • HY-110279
    Ogerin

    Others Neurological Disease
    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
  • HY-135909
    TH1217

    ZINC1775962367

    SARS-CoV Cancer Infection
    TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
  • HY-W009204S5
    Fmoc-Ala-OH-13C3

    PPAR Metabolic Disease
    Fmoc-Ala-OH-13C3 is a 13C-labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-ind
  • HY-134494
    MS48107

    Others Neurological Disease
    MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
  • HY-119226
    VU0152099

    mAChR Neurological Disease
    VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
  • HY-P1303A
    CART(62-76)(human,rat) TFA

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • HY-122590
    Glabrescione B

    Gli Cancer
    Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
  • 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-120717
    VU6001966

    mGluR Others
    VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer.
  • HY-146389
    Anticancer agent 50

    MDM-2/p53 P-glycoprotein Cancer
    Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    Others Others
    Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
  • HY-12158
    VU0238441

    mAChR Neurological Disease
    VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.
  • HY-12150
    CCMI

    AVL-3288; UCI-4083

    nAChR Neurological Disease
    CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
  • HY-B0282S
    Acetylcholine-d4 chloride

    ACh-d4 chloride

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d9 (ACh-d9) chloride is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.
  • HY-122559
    BMS-984923

    mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
  • HY-P2076
    Dusquetide

    SGX942

    Bacterial Cancer Infection
    Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-120789
    PF-06648671

    γ-secretase Neurological Disease
    PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
  • HY-16579AS2
    Etifoxine-d5

    GABA Receptor Neurological Disease
    Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-16579AS
    Etifoxine-d3

    GABA Receptor Neurological Disease
    Etifoxine-d3 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
  • HY-B0282S1
    Acetylcholine-d9 chloride

    ACh-d9 chloride

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d9 (ACh-d9) chloride is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.
  • HY-19888
    GSK-1482160

    P2X Receptor Inflammation/Immunology
    GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases.
  • HY-104037
    Cintirorgon

    LYC-55716

    ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • HY-142942
    Glucocorticoid receptor-IN-2

    Glucocorticoid Receptor MMP Inflammation/Immunology
    Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV.
  • HY-112257
    S-23

    Androgen Receptor Metabolic Disease
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
  • HY-N0313
    Euphol

    Endogenous Metabolite MAGL Inflammation/Immunology
    Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
  • HY-136866
    Aβ42-IN-2

    γ-secretase Neurological Disease
    Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of Alzheimer's disease.
  • HY-P2264
    KYL peptide

    Ephrin Receptor Inflammation/Immunology
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-115670
    GW280264X

    MMP Cancer Inflammation/Immunology
    GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells.
  • HY-103524
    Valerenic acid

    (-)-Valerenic Acid

    GABA Receptor 5-HT Receptor Neurological Disease
    Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-131019
    JF-NP-26

    mGluR Neurological Disease
    JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-132189
    Laniquidar

    R101933

    P-glycoprotein Cancer
    Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters. Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Laniquidar has limited oral bioavailability.
  • HY-B0723S
    Ospemifene D4

    FC-1271a D4

    Estrogen Receptor/ERR Cancer
    Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
  • HY-117639
    AUT1

    Potassium Channel Cancer
    AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
  • HY-101064S1
    Fmoc-leucine-13C6,15N

    PPAR Metabolic Disease
    Fmoc-leucine-13C6,15N is a 15N-labeled and 13C-labled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity
  • HY-129636
    (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-N2499
    Dehydrotumulosic acid

    Others Metabolic Disease
    Dehydrotumulosic acid is one of the effective constituents of Poria cocos. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body.
  • HY-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
  • HY-N6843
    Arnicolide D

    Caspase PI3K Akt mTOR STAT Cancer
    Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
  • HY-P2076A
    Dusquetide TFA

    SGX942 TFA

    Bacterial Cancer Infection
    Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-126327
    UNC4976

    Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-N7695
    Physalin B

    Apoptosis Autophagy Cancer
    Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro.
  • HY-118861
    Enclomiphene

    (E)-Clomiphene; trans-Clomiphene; Enclomifene

    Estrogen Receptor/ERR Endocrinology Metabolic Disease
    Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
  • HY-118861B
    Enclomiphene hydrochloride

    (E)-Clomiphene hydrochloride; trans-Clomiphene hydrochloride; Enclomifene hydrochloride

    Estrogen Receptor/ERR Endocrinology Metabolic Disease
    Enclomiphene ((E)-Clomiphene) hydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene hydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
  • HY-118861A
    Enclomiphene citrate

    (E)-Clomiphene citrate; trans-Clomiphene citrate; Enclomifene citrate

    Estrogen Receptor/ERR Endocrinology Metabolic Disease
    Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene citrate can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
  • 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-B0116
    Stavudine

    d4T

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
  • HY-B0116A
    Stavudine sodium

    d4T sodium

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.
  • HY-B0723S1
    Ospemifene-d4-1

    FC-1271a-d4-1

    Estrogen Receptor/ERR Cancer
    Ospemifene-d4-1 (FC-1271a-d4-1) is the deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
  • HY-147855
    ACA-28

    ERK Apoptosis Cancer
    ACA-28 (compound 2a) is a potent ERK MAPK signaling modulator. ACA-28 selectively inhibits cancer cell growth by inducing apoptosis with ERK hyperactivation ACA-28 inhibits cell growth of melanoma cells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively.
  • HY-116785
    BRD32048

    DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen.
  • HY-105115
    Abecarnil

    ZK 112119

    GABA Receptor Neurological Disease
    Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
  • HY-106225
    Rotigaptide

    ZP123

    Gap Junction Protein Cardiovascular Disease
    Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
  • HY-143874
    HER2-IN-7

    EGFR Cancer
    HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23).
  • HY-116247
    ST247

    PPAR Metabolic Disease Inflammation/Immunology
    ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ.
  • HY-W011733
    Tulobuterol hydrochloride

    C-78

    Adrenergic Receptor Influenza Virus Antibiotic Infection Endocrinology Inflammation/Immunology
    Tulobuterol hydrochloride (C-78) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol hydrochloride is also a sympathomimetic agent used as a transdermal patch, increases normal diaphragm muscle strength. Tulobuterol hydrochloride inhibit rhinovirus replication and modulate airway inflammation.
  • HY-144119
    Cas9-IN-2

    CRISPR/Cas9 Others
    Cas9-IN-2 is a potent Cas9 inhibitor (IC50=246 μM), Cas9-IN-2 acts by binding to apo-Cas9 to prevent Cas9:gRNA complex formation, which can potentially be applied to modulate and control Cas9 activity in various applications.
  • HY-P1397A
    RVD-Hpα TFA

    Cannabinoid Receptor
    RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-110162
    QO 58

    Potassium Channel Neurological Disease
    QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability.
  • HY-101064S3
    Fmoc-leucine-d10

    PPAR
    Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity.
  • HY-123671
    CYM2503

    Neuropeptide Y Receptor Neurological Disease
    CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy.
  • HY-131337
    RhlR antagonist 1

    Bacterial Infection
    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.
  • HY-P1216
    HS014

    Melanocortin Receptor Neurological Disease
    HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
  • HY-10016
    E 2012

    γ-secretase Neurological Disease
    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-B2163
    Astaxanthin

    PPAR Reactive Oxygen Species Endogenous Metabolite Cancer Cardiovascular Disease
    Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
  • HY-116463B
    (2S,3S)-E1R

    Sigma Receptor Neurological Disease
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-121508
    (E/Z)-IT-603

    NF-κB Cancer Inflammation/Immunology
    (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
  • HY-101064S2
    Fmoc-leucine-d3

    N-FMOC-leucine-d3; NPC 15199-d3; NSC 334290-d3

    PPAR
    Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity.
  • HY-116463A
    (2R,3S)-E1R

    Sigma Receptor Neurological Disease
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-12152
    PNU-120596

    NSC 216666

    nAChR Inflammation/Immunology Neurological Disease
    PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
  • HY-116463C
    (2R,3R)-E1R

    Sigma Receptor Neurological Disease
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-103118
    PU02

    5-HT Receptor Apoptosis Cancer Neurological Disease
    PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
  • HY-102070
    NS13001

    Potassium Channel Neurological Disease
    NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
  • HY-139644
    MIPS521

    Adenosine Receptor Neurological Disease
    MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.
  • HY-B0005S
    Toremifene-d6 citrate

    Estrogen Receptor/ERR Apoptosis Cancer Infection
    Toremifene-d6 (Z-Toremifene-d6) citrate is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
  • HY-P1216A
    HS014 TFA

    Melanocortin Receptor Neurological Disease
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
  • HY-143792
    HTT-D3

    P-glycoprotein Neurological Disease
    HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research.
  • HY-12005
    Fingolimod hydrochloride

    FTY720

    LPL Receptor PAK Inflammation/Immunology Cancer
    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-32067
    Aceclidine

    Quinuclidin-3-yl acetate

    mAChR Neurological Disease
    Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia (extracted from patent US20150290125A1/US20110091459A1).
  • HY-101292
    FK614

    PPAR Metabolic Disease
    FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.
  • HY-100348
    EPI-001

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-145196
    RTICBM-189

    Cannabinoid Receptor Neurological Disease
    RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats.
  • HY-118689
    RA-2

    Potassium Channel Inflammation/Immunology Neurological Disease Cardiovascular Disease
    RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation.
  • HY-113066
    Guanosine 5'-diphosphate

    GDP

    Endogenous Metabolite Potassium Channel Inflammation/Immunology
    Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
  • HY-122255
    LY487379

    mGluR Neurological Disease
    LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.
  • HY-107508
    VU-29

    mGluR Neurological Disease
    VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
  • HY-128895
    KL1333

    Mitochondrial Metabolism Metabolic Disease
    KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures.
  • HY-103457
    Y134

    Estrogen Receptor/ERR Cancer
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
  • HY-B0116S
    Stavudine-d4

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
  • HY-130609
    Aβ42-IN-1

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-106901AS
    Asoxime-d4 dichloride

    HI-6-d4

    nAChR Neurological Disease
    Asoxime-d4 dichloride (HI-6-d4) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • HY-16560
    Camptothecin

    Campathecin; (S)-(+)-Camptothecin; CPT

    Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Cancer Infection
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
  • HY-100490B
    Rilmenidine phosphate

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Cardiovascular Disease
    Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
  • HY-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-B1640
    Ethacrynic acid

    Etacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-15671
    GKA50

    Glucokinase Metabolic Disease
    GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
  • HY-100490
    Rilmenidine

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Cardiovascular Disease
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one

    THDOC

    GABA Receptor Neurological Disease
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-N0411
    β-Carotene

    Provitamin A; beta-Carotene

    Endogenous Metabolite Apoptosis Reactive Oxygen Species Cancer Metabolic Disease
    β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
  • HY-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • HY-P1075
    CALP3

    Calcium Channel Cancer Neurological Disease
    CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-19620A
    Branaplam hydrochloride

    LMI070 hydrochloride; NVS-SM1 hydrochloride

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-19620
    Branaplam

    LMI070; NVS-SM1

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-100604
    JNJ-40418677

    γ-secretase Amyloid-β Neurological Disease
    JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-A0031S1
    Bazedoxifene-d4 N-Oxide

    Estrogen Receptor/ERR Cancer
    Bazedoxifene-d4 N-Oxide is the deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-118140
    ZCZ011

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain.
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-103552
    LY487379 hydrochloride

    mGluR Neurological Disease
    LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt

    GDP disodium salt

    Endogenous Metabolite Potassium Channel Inflammation/Immunology
    Guanosine 5'-diphosphate (GDP) disodium salt is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate disodium salt can be used in the research of inflammation, such as anemia of inflammation (AI).
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-15672
    FM19G11

    HIF/HIF Prolyl-Hydroxylase Cancer Neurological Disease
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-146399
    AChE/BChE-IN-9

    Cholinesterase (ChE) ROS Kinase Neurological Disease
    AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB.
  • HY-119695AS
    Simvastatin acid-d6 ammonium

    Tenivastatin-d6 ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin acid-d6 (Tenivastatin-d6) ammoniumis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-125390
    SM-360320

    CL-087

    Toll-like Receptor (TLR) Inflammation/Immunology
    SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
  • HY-P0063
    Copper tripeptide

    GHK-Cu

    Endogenous Metabolite Inflammation/Immunology
    Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
  • HY-100490A
    Rilmenidine hemifumarate

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Cardiovascular Disease
    Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
  • HY-B1805S
    Triclocarban-d4

    3,4,4′-Trichlorocarbanilide-d4

    Bacterial Infection
    Triclocarban-d4 (3,4,4′-Trichlorocarbanilide-d4) is the deuterium labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes.
  • HY-15671A
    GKA50 quarterhydrate

    Glucokinase Metabolic Disease
    GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
  • HY-134050
    Apostatin-1

    Apt-1

    RIP kinase Autophagy Apoptosis Beclin1 Necroptosis Inflammation/Immunology
    Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin.
  • HY-111751
    JNJ-61432059

    iGluR Neurological Disease
    JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.
  • HY-110143
    CLP257

    Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
  • HY-A0031S
    Bazedoxifene-d4

    TSE-424-d4

    Estrogen Receptor/ERR Cancer
    Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-P1075A
    CALP3 TFA

    Calcium Channel Cancer Neurological Disease
    CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-13456
    LY-404187

    iGluR Neurological Disease
    LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
  • HY-135276
    Targaprimir-96

    MicroRNA Apoptosis Cancer
    Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-P1218
    Phrixotoxin 3

    Sodium Channel Neurological Disease
    Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-120355A
    AP14145 hydrochloride

    Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
  • HY-12700
    RO5256390

    Others Neurological Disease
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
  • HY-105231
    Bryostatin 1

    PKC HIV Cancer Infection Inflammation/Immunology Neurological Disease
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
  • HY-100490S
    Rilmenidine-d4

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Cardiovascular Disease
    Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-10241
    Simeprevir

    TMC435; TMC435350

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • HY-16560S
    Camptothecin-d5

    Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5

    Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Cancer Infection
    Camptothecin-d5 (Campathecin-d5) is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
  • HY-12355
    Siponimod

    BAF-312

    LPL Receptor Inflammation/Immunology Neurological Disease
    Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research -.
  • HY-121618
    α-Thujone

    GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-131032
    KI-7

    Adenosine Receptor Others
    KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively.
  • HY-117482
    BPN-15606

    γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-16023
    Acolbifene hydrochloride

    EM-652 hydrochloride; SCH 57068 hydrochloride

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
  • HY-10241A
    Simeprevir sodium

    TMC435 sodium; TMC435350 sodium

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • HY-135276A
    Targaprimir-96 TFA

    MicroRNA Apoptosis Cancer
    Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-12355A
    Siponimod hemifumarate

    BAF-312 hemifumarate

    LPL Receptor Inflammation/Immunology Neurological Disease
    Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-100588
    VU0364770

    mGluR Neurological Disease
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-141431
    Cbl-b-IN-2

    E3 Ligase Ligand-Linker Conjugates Cancer Inflammation/Immunology
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
  • HY-130344
    SKF83959

    Dopamine Receptor Sigma Receptor Neurological Disease
    SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.
  • HY-110155
    LM11A-31 dihydrochloride

    Others Neurological Disease
    LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
  • HY-143880
    MRGPRX1 agonist 4

    Others Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.
  • HY-P1218A
    Phrixotoxin 3 TFA

    Sodium Channel Neurological Disease
    Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-121140
    AZ1729

    Others Metabolic Disease
    AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-W063968
    RO8191

    CDM-3008; RO4948191

    IFNAR JAK STAT HCV HBV Infection
    RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
  • HY-14571
    E7820

    ER68203-00

    Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-136258
    nAChR agonist CMPI hydrochloride

    nAChR Neurological Disease
    nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
  • HY-117482A
    BPN-15606 besylate

    γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-100588A
    VU0364770 hydrochloride

    mGluR Neurological Disease
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-B1803A
    Tracazolate hydrochloride

    ICI 136753 hydrochloride

    GABA Receptor Neurological Disease
    Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
  • HY-113008AS
    cis-Urocanic acid-13C3

    (Z)-Urocanic acid-13C3; cis-UCA-13C3

    5-HT Receptor Inflammation/Immunology
    cis-Urocanic Acid-13C3 ((Z)-Urocanic acid-13C3) is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
  • HY-100991
    FG 7142

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
  • HY-B0008
    Sulindac

    MK-231

    COX Autophagy Inflammation/Immunology Cancer
    Sulindac is an FDA-approved orally active nonsteroidal anti-inflammatory agent. Sulindac, as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1.
  • HY-103552S
    LY487379-d3 hydrochloride

    mGluR Neurological Disease
    LY487379-d3 hydrochloride is the deuterium labeled LY487379 hydrochloride. LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research.
  • HY-17606
    Cenerimod

    ACT-334441

    LPL Receptor Inflammation/Immunology
    Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
  • HY-145015
    HM43239

    FLT3 Apoptosis Cancer
    HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells.
  • HY-70057
    Safinamide

    FCE 26743; EMD 1195686

    Monoamine Oxidase Neurological Disease
    Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-108022A
    MSDC-0602K

    Azemiglitazone potassium

    Insulin Receptor PPAR Metabolic Disease
    MSDC-0602K (Azemiglitazone potassium), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM. MSDC-0602K modulates the mitochondrial pyruvate carrier (MPC). MSDC-0602K can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance. MSDC-0602K, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide.
  • HY-135581S
    Raloxifene 6-glucuronide-d4

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 is the deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-133910
    Lu AE98134

    Sodium Channel Neurological Disease
    Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.
  • HY-135581S1
    Raloxifene 6-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-B0008A
    Sulindac sodium

    MK-231 sodium

    NF-κB PD-1/PD-L1 Sirtuin Cancer Infection Inflammation/Immunology
    Sulindac (sodium) (MK-231 (sodium)) is an FDA-approved orally active nonsteroidal anti-inflammatory agent. Sulindac, as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) (MK-231 (sodium)) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1.
  • HY-135582S1
    Raloxifene 4'-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-70057A
    Safinamide mesylate

    FCE 26743 mesylate; EMD 1195686 mesylate

    Monoamine Oxidase Neurological Disease Cardiovascular Disease
    Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.
  • HY-103412
    SKF 83959 hydrobromide

    Dopamine Receptor Sigma Receptor Neurological Disease
    SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression.
  • HY-116818
    Crebinostat

    HDAC Neurological Disease
    Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice.
  • HY-134557
    GS87

    GSK-3 Cancer
    GS87 is a highly specific and potent GSK3 inhibitor with IC50s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research.
  • HY-113466S
    4-Hydroxynonenal-d3

    4-HNE-d3

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal-d3 (4-HNE-d3) is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-108511
    PB28 dihydrochloride

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.
  • HY-12403A
    Angiotensin (1-7) (acetate)

    Ang-(1-7) (acetate)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Endocrinology Inflammation/Immunology Cardiovascular Disease
    Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium.
  • HY-70057S1
    Safinamide-d4-1

    FCE 26743-d4-1; EMD 1195686-d4-1

    Monoamine Oxidase Neurological Disease
    Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-10241S
    Simeprevir-13C,d3

    TMC435-13C,d3; TMC435350-13C,d3

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir-13C,d3 (TMC435-13C,d3) is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • HY-12403
    Angiotensin (1-7)

    Ang-(1-7)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Endocrinology
    Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
  • HY-70057S
    Safinamide-d4

    Monoamine Oxidase Neurological Disease
    Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-N0281
    Daphnetin

    7,8-Dihydroxycoumarin

    EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite Inflammation/Immunology Cancer
    Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
  • HY-103066
    Br-PBTC

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel Neurological Disease
    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals.
  • HY-123489S
    3α,21-Dihydroxy-5α-pregnan-20-one-d3

    THDOC-d3

    GABA Receptor Neurological Disease
    3α,21-Dihydroxy-5α-pregnan-20-one-d3 (THDOC-d3) is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-109112
    Brilaroxazine

    RP5063

    Dopamine Receptor 5-HT Receptor Inflammation/Immunology Neurological Disease
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
  • HY-131997
    2'MeO6MF

    GABA Receptor Inflammation/Immunology Neurological Disease
    2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
  • HY-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.