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Results for "

Allosteric ampk Inhibitors

" in MedChemExpress (MCE) Product Catalog:

781

Inhibitors & Agonists

5

Screening Libraries

3

Biochemical Assay Reagents

26

Peptides

1

Inhibitory Antibodies

57

Natural
Products

8

Recombinant Proteins

29

Isotope-Labeled Compounds

11

Antibodies

9

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas
  • HY-151361
    AMPK-IN-3
    1 Publications Verification

    		 AMPK Cancer
    AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer.
  • HY-117623
    PF-06685249

    PF-249

    		 AMPK Metabolic Disease
    PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 can be used for diabetic nephropathy research.
  • HY-155363
    AMPK activator 13

    		AMPK Metabolic Disease
    AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity.
  • HY-154973
    AMPK activator 11

    		Mitochondrial Metabolism AMPK Cancer Metabolic Disease
    AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research.
  • HY-147037
    AMPK activator 7

    		AMPK Metabolic Disease Cardiovascular Disease
    AMPK activator 7 (compound I-3-24) is a an AMPK activator with the EC50 of 8.8 nM. AMPK activator 7 can be used for the research of diseases involving AMPK, particularly diseases such as type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia and/or hypertension.
  • HY-146398
    AMPK activator 6

    		AMPK Metabolic Disease
    AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.
  • HY-150056
    CB1R Allosteric modulator 3

    		Cannabinoid Receptor Arrestin Neurological Disease
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.
  • HY-120904
    AMPK-IN-1

    		AMPK Metabolic Disease
    AMPK-IN-1 is an activator of AMPK (EC50: 551 nM for isoform α2β2γ1). AMPK-IN-1 leads to eEF2 phosphorylation in a mTORC1-independent way.
  • HY-150057
    CB1R Allosteric modulator 4

    		Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.
  • HY-148684
    AMPK activator 10

    		AMPK Metabolic Disease
    AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect.
  • HY-131334
    AMPK activator 4

    		AMPK Metabolic Disease
    AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
  • HY-149406
    AMPK activator 12

    		AMPK Cancer
    AMPK activator 12 (compound 21) is a potent AMPK activator and GDF15 inducer. AMPK activator 12 increases GDF15 protein levels in human hepatic cells.
  • HY-148210
    AMPK activator 9

    		AMPK Metabolic Disease
    AMPK activator 9 (ZM-6) is a potent AMPK (α2β1γ1) activator with an EC50 value of 1.1 µM. AMPK activator 9 has the potential for the research of type 2 diabetes.
  • HY-U00292
    AMPK activator 1

    		AMPK Metabolic Disease
    AMPK activator 1 is an AMPK activator extracted from patent WO2013116491A1, compound No.1-75, has an EC50 of <0.1μM.
  • HY-130723
    AMPK activator 2

    		AMPK Cancer
    AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549).
  • HY-130723A
    AMPK activator 2 hydrochloride

    		AMPK Cancer
    AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549).
  • HY-155967
    CB1R/AMPK modulator 1

    		Cannabinoid Receptor AMPK Metabolic Disease
    CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity.
  • HY-147038
    AMPK activator 8

    		AMPK Metabolic Disease
    AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.
  • 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-147653
    Integrase-LEDGF/p75 allosteric inhibitor 1

    		HIV Integrase Infection
    Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432.
  • HY-157129
    AMPK-α1β1γ1 activator 1

    		AMPK Cardiovascular Disease
    AMPK-α1β1γ1 activator 1 (M1) is an acyl glucuronide metabolite of Indole-3-carboxylic Acid-based AMPK activator. AMPK-α1β1γ1 activator 1 can selectively activated human β1 isoforms with an EC50 value of 38.1nM. AMPK-α1β1γ1 activator 1 can direct binding with human AMPK α1β1γ1 isoform. AMPK-α1β1γ1 activator 1 can be used for the research of diabetic nephropathy.
  • HY-N9349
    Malvidin-3-O-arabinoside chloride

    		AMPK Autophagy Metabolic Disease Inflammation/Immunology
    Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy.
  • HY-N4253
    Kudinoside D

    		Others Metabolic Disease
    Kudinoside D is a main natural component of triterpenoid saponin derived from Ilex kudingcha. Kudinoside D suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.
  • HY-16708A
    ZLN024 hydrochloride
    1 Publications Verification

    		 AMPK Metabolic Disease
    ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-16708
    ZLN024

    		AMPK Metabolic Disease
    ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
  • HY-N11924
    Foenumoside B

    		PPAR AMPK Metabolic Disease
    Foenumoside B is a triterpene saponin isolated from Lysimachia foenum-graecum. Foenumoside B activates AMPK signaling, inhibits PPARγ-induced adipogenesis, and shifts lipid metabolism toward lipolysis. Foenumoside B can be used in the study of obesity and obesity-related metabolic diseases.
  • HY-103683
    PF-06409577

    		AMPK Metabolic Disease
    PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
  • HY-A0144A
    Etilefrine hydrochloride

    		Adrenergic Receptor AMPK Cardiovascular Disease
    Etilefrine hydrochloride is an orally active α adrenergic agonist. Etilefrine hydrochloride is also an AMPK activator. Etilefrine hydrochloride can be used for the research of postural hypotension.
  • HY-148249
    NVS-MALT1

    		MALT1 Cancer
    NVS-MALT1 is a MALT1 allosteric inhibitor.
  • HY-153975
    SIK2-IN-1

    		Salt-inducible Kinase (SIK) Cancer Inflammation/Immunology
    SIK2-IN-1 (compound 8g) is a potent SIK2 inhibitor over other AMPK kinases. SIK2-IN-1 exhibits favorable in vitro ADMET profiles and decent cellular activities.
  • HY-103238
    RSVA405

    		AMPK STAT Autophagy Metabolic Disease Inflammation/Immunology Neurological Disease
    RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.
  • HY-A0144
    Etilefrine

    		Adrenergic Receptor AMPK Cardiovascular Disease
    Etilefrine (3-[2-(ethylamino)-1-hydroxyethyl]phenol) is an α adrenergic agonist. Etilefrine also is an AMPK activator. Etilefrine can be used for the research of postural hypotension.
  • HY-119806
    TMPPAA

    		5-HT Receptor Neurological Disease
    TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling.
  • HY-124822
    COH-SR4

    		AMPK Cancer Metabolic Disease
    COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.
  • HY-N6077
    Thalidezine

    		Others Cancer
    Thalidezine is a novel activator of AMP-activated protein kinase (AMPK). Thalidezine can eliminate anti-apoptotic cancer cells through energy-mediated autophagy death. Thalidezine can be used to study apoptosis intervention .
  • HY-103503
    CGP13501

    		GABA Receptor Neurological Disease
    CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol.
  • HY-119765
    VU0366248

    		mGluR Neurological Disease
    VU0366248 is a mGlu5 negative allosteric modulator.
  • HY-121879
    SHP836
    1 Publications Verification

    		 SHP2 Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-141543
    YW2065

    		β-catenin Cancer
    YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPK activation.
  • HY-W017212
    Methyl cinnamate

    Methyl 3-phenylpropenoate

    		 Tyrosinase Bacterial AMPK Infection Metabolic Disease
    Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
  • HY-116067
    VU0404251

    		mGluR Neurological Disease
    U0404251 is a highly potent positive allosteric modulator of mGlu for the study of psychosis.
  • HY-110087
    4BP-TQS

    		nAChR Neurological Disease
    4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site.
  • HY-103497
    U-89843A

    		GABA Receptor Neurological Disease
    U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl - currents.
  • HY-14691
    Refametinib
    10+ Cited Publications

    BAY 869766; RDEA119

    		 MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
  • HY-W011012
    Adenosine 5'-monophosphate disodium
    5 Publications Verification

    		 Adenosine Receptor Metabolic Disease
    Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes.
  • HY-155467
    MRS7935

    		Adenosine Receptor Endocrinology
    MRS7935 (compound 15) is an A1AR positive allosteric modulator (PAM) with an EC50 of approximately 2 μM.
  • HY-W013816
    Dipentyl phthalate

    		Akt AMPK Metabolic Disease
    Dipentyl phthalate is an endocrine-disrupting phthalate plasticizer. Dipentyl phthalate increases AMPK phosphorylation and decreases AKT1 phosphorylation and SIRT1 levels. Dipentyl phthalate reduces adrenocorticotropic hormone levels. Dipentyl phthalate is a testicular toxicant.
  • 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-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-N7676
    Marein

    		AMPK HDAC Metabolic Disease Neurological Disease Cardiovascular Disease
    Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
  • HY-144690
    D5261

    		Trk Receptor Cancer
    D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
  • HY-10915
    LUF6096

    		Adenosine Receptor Cardiovascular Disease
    LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.
  • 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-122819
    Calindol hydrochloride

    		CaSR Cardiovascular Disease
    Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM.
  • HY-13236
    LUF6000
    1 Publications Verification

    		 Adenosine Receptor Cardiovascular Disease
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
  • HY-125355
    SEC

    		Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • 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-13418G
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 dihydrochloride

    		 AMPK Cancer Neurological Disease
    Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs).
  • 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-107587
    A-286982
    1 Publications Verification

    		 Integrin Inflammation/Immunology
    A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively.
  • 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-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-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-143656
    SH379

    		Autophagy Endocrinology
    SH379 is the derivative of 2-methylpyrimidine-fused tricyclic diterpene. SH379 is a potent and orally active anti-late-onset hypogonadism agent. SH379 significantly promotes the expression of the key testosterone synthesis-related enzymes StAR and 3β-HSD. SH379 stimulates autophagy through regulating AMPK/mTOR signaling pathway.
  • HY-135805A
    (Rac)-JBJ-04-125-02

    		EGFR Cancer
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor.
  • HY-109128
    Danicamtiv

    MYK-491

    		 Myosin Cancer
    Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
  • HY-118806
    AC-42

    		mAChR Neurological Disease
    AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively.
  • 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-19330
    DASA-58
    10+ Cited Publications

    		 Pyruvate Kinase Cancer Metabolic Disease
    DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer.
  • HY-114397
    SHP394

    		SHP2 Phosphatase Cancer
    SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.
  • HY-150210
    FSHR agonist 1

    		Estrogen Receptor/ERR Endocrinology
    FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR.
  • 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-139399
    Safimaltib

    JNJ-67856633

    		 MALT1 Cancer
    Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.
  • 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. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression.
  • 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-139303
    LUF5771

    		Others Endocrinology
    LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy.
  • HY-B2099
    Buformin

    1-Butylbiguanide

    		 AMPK Cancer Metabolic Disease
    Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
  • HY-B2099A
    Buformin hydrochloride
    2 Publications Verification

    1-Butylbiguanide hydrochloride

    		 AMPK Cancer
    Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
  • 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-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-110286
    6-Hydroxy-DOPA

    		DNA/RNA Synthesis Cancer
    6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer.
  • 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-137820
    Brr2-IN-3

    		Others Others
    Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM.
  • HY-100953
    CYM-5520

    		LPL Receptor Metabolic Disease
    CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research.
  • HY-10933
    CX516
    1 Publications Verification

    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-14563
    VU10010

    		mAChR Neurological Disease
    VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
  • HY-145159
    SHP2 protein degrader-1

    		SHP2 PROTACs Phosphatase Apoptosis Cancer
    SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases.
  • 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-103693
    NAZ2329

    		Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-112769
    EX229
    2 Publications Verification

    		 AMPK Metabolic Disease
    EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
  • HY-103574
    Raseglurant hydrochloride

    ADX-10059 hydrochloride

    		 mGluR Neurological Disease
    Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine.
  • HY-143312
    V-0219

    		GLP Receptor 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-107504
    VU0360172 hydrochloride

    		mGluR Neurological Disease
    VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice.
  • HY-17592
    Bithionol
    1 Publications Verification

    		 Parasite Bacterial Cancer Infection
    Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM).
  • HY-141520
    ART558
    5+ Cited Publications

    		 DNA/RNA Synthesis Cancer
    ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.
  • HY-132265
    SCO-267
    2 Publications Verification

    		 Free Fatty Acid Receptor Metabolic Disease
    SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes.
  • HY-144291
    LY3154885

    		Dopamine Receptor Neurological Disease
    LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent 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-143345
    EN523

    		Others Cancer
    EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1.
  • HY-P2952
    Adenylate

    ampk; Myokinase; Adk

    		 Endogenous Metabolite Others
    Adenylate (Adk), i.e., myokinase, is a phosphotransferase enzyme, is often used in biochemical studies. Adenylate catalyzes the interconversion of adenosine phosphates. Adenylate monitors phosphate nucleotide levels inside the cell, it plays an important role in cellular energy homeostasis.
  • 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-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-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-147260B
    (Rac)-Dalzanemdor

    (Rac)-SAGE-718

    		 TRP Channel Neurological Disease
    (Rac)-Dalzanemdor ((Rac)-SAGE-718) is an isomer of Dalzanemdor (HY-147260). Dalzanemdor is an orally active and highly intrinsically active N-methyl-d-aspartate receptor (NMDAR)-positive allosteric modulator (PAM). Dalzanemdor can be used in the research of Huntington's disease.
  • 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-103239
    PT1

    		AMPK Metabolic Disease Cardiovascular Disease
    PT1 is an AMPKα1 activator that directly activates the inactive truncated forms of AMPKα1 monomers.
  • HY-12357
    Bempedoic acid
    5+ Cited Publications

    ETC-1002; ESP-55016

    		 ATP Citrate Lyase AMPK Metabolic Disease
    Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.
  • HY-N6913
    3α-Hydroxymogrol

    		AMPK Metabolic Disease
    3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
  • HY-19934
    Pifusertib

    TAS-117

    		 Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy.
  • HY-19934A
    Pifusertib hydrochloride

    TAS-117 hydrochloride

    		 Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy.
  • HY-120270
    PF-06679142

    		AMPK Metabolic Disease
    PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC50 of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research.
  • HY-118160
    PPM-18

    NSC 73233

    		 NO Synthase Inflammation/Immunology Cancer
    PPM-18 (NSC 73233), a potent anti-inflammatory agent, inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter. PPM-18, an analog of Vitamin K, induces autophagy and apoptosis in bladder cancer cells through ROS and AMPK signaling pathways.
  • 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-113689
    GAT211

    		Cannabinoid Receptor Neurological Disease
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.
  • HY-155148
    MAT2A-IN-11

    		Methionine Adenosyltransferase (MAT) Cancer
    MAT2A Allosteric inhibitor 1 (compound 5) is a MAT2A selective inhibitor of methionine adenosyltransferase (MAT) with an IC50 of 6.8 nM.
  • HY-120428
    VU0410425

    		mGluR Neurological Disease
    VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders.
  • 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-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-119339
    SX-682
    3 Publications Verification

    		 CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • 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-11007
    GNF-2
    2 Publications Verification

    		 Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-121140
    AZ1729

    		Free Fatty Acid Receptor 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-143899
    FBA-IN-1

    		Fungal Infection
    FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL.
  • 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 addictive agent-seeking behavior in rats.
  • 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-106199
    Adenosine A1 receptor activator T62
    1 Publications Verification

    		 Adenosine Receptor Inflammation/Immunology Neurological Disease
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
  • HY-130000
    Pirmitegravir

    STP0404

    		 HIV Integrase HIV Infection
    Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
  • HY-124805
    MAL3-101

    		HSP Cancer
    MAL3-101 is a potent HSP70 allosteric inhibitor. MAL3-101 inhibits HSP70 ATPase activity by blocking Hsp40 co-chaperone interaction. MAL3-101 can be used for researching muscle invasive bladder cancer (MIBC).
  • 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
    Levamisole
    3 Publications Verification

    (-)-Tetramisole

    		 nAChR Parasite Infection Inflammation/Immunology Cancer
    Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. 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-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-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-115553
    DETQ

    		Dopamine Receptor Neurological Disease
    DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
  • HY-12357S2
    Bempedoic acid-d4

    ETC-1002-d4; ESP-55016-d4

    		 ATP Citrate Lyase AMPK Others
    Bempedoic acid-d4 is the deuterium labeled Bempedoic acid. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK[1][2].
  • HY-117755
    PF-739

    		AMPK Metabolic Disease
    PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.
  • 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-15701B
    ADH-503

    (Z)-Leukadherin-1 choline

    		 Complement System Cancer
    ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • 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-133128
    FM26

    		ROR Cancer
    FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
  • 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-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-15701A
    (Z)-Leukadherin-1

    ADH-503 free base

    		 Complement System Cancer
    (Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-111363
    MK8722
    5+ Cited Publications

    		 AMPK Metabolic Disease
    MK8722 is a potent and systemic pan-AMPK activator.
  • HY-119464
    MRL-871

    		ROR Cancer
    MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 12.7 nM. MRL-871 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
  • HY-136173
    Batoprotafib
    2 Publications Verification

    TNO155

    		 SHP2 Phosphatase Cancer
    Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • 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. ML289 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-12357S
    Bempedoic acid-d5

    ETC-1002-d5; ESP-55016-d5

    		 ATP Citrate Lyase AMPK Metabolic Disease
    Bempedoic acid-d5 is the deuterium labeled Bempedoic acid[1]. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2].
  • 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-12831
    Ampkinone
    1 Publications Verification

    		 AMPK Metabolic Disease
    Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator.
  • HY-133073
    CCR7 Ligand 1

    CCR7-Cmp2105

    		 CCR Ligands for Target Protein for PROTAC Cancer
    CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
  • HY-136789
    Tuxobertinib

    BDTX-189

    		 EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  • HY-P0136
    SAMS
    2 Publications Verification

    		 AMPK Metabolic Disease
    SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
  • HY-N5018
    Nepodin

    Musizin

    		 Parasite AMPK Infection
    Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus.Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK.Nepodin (Musizin) has antidiabetic and antimalarial activities.
  • HY-115669
    Pentachloropseudilin

    Antibiotic A 15104 Y; PClP

    		 Myosin TGF-β Receptor Cancer
    Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β.
  • 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-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. ML337 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-148510
    HKB99

    		Phosphatase Cancer
    HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 inhibits the formation of invasive pseudopodia and increases the level of PAI-2 in vitro. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC).
  • HY-100388B
    SHP099 hydrochloride

    		SHP2 Cancer
    SHP099 hydrochloride is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2 D61Y, SHP2E69K, SHP2 A72V, SHP2 E76K. SHP099 hydrochloride inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 hydrochloride inhibits RAS-ERK signaling and inhibit tumor growth.
  • HY-103111
    MMPIP hydrochloride

    		mGluR Neurological Disease
    MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • HY-107503
    MMPIP

    		mGluR Neurological Disease
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • HY-103320A
    Calhex 231 hydrochloride
    2 Publications Verification

    		 CaSR Metabolic Disease
    Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • 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-103565
    AMN082

    		mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-114011
    AMG7703

    		Free Fatty Acid Receptor Metabolic Disease Inflammation/Immunology
    AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic.
  • HY-112233
    O-304
    3 Publications Verification

    		 AMPK Metabolic Disease Cardiovascular Disease
    O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a agent to treat type 2 diabetes (T2D) and associated cardiovascular complications .
  • 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-50662
    A-769662
    20+ Cited Publications

    		 AMPK Cancer
    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
  • HY-16397A
    Phenformin hydrochloride
    5+ Cited Publications

    Phenethylbiguanide hydrochloride

    		 AMPK Autophagy Cancer
    Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity.
  • HY-120877
    MRT199665

    		Salt-inducible Kinase (SIK) AMPK Apoptosis Cancer
    MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
  • 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-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-agent like properties and clinical candidate potential. .
  • HY-103565A
    AMN082 free base

    		mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • 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-153699
    SHP2-IN-14

    		SHP2 Cancer
    SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty.
  • HY-103076
    EZ-482
    1 Publications Verification

    		 Others Neurological Disease
    EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas.
  • 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-107988
    MK-3903
    2 Publications Verification

    		 AMPK Metabolic Disease
    MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
  • HY-N6631
    7-Methoxyisoflavone
    2 Publications Verification

    		 AMPK Metabolic Disease Cancer
    7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).
  • HY-15840
    YLF-466D
    2 Publications Verification

    C24

    		 AMPK Cancer
    YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
  • HY-50672
    MK-0731

    		Kinesin Apoptosis Cancer
    MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy.
  • HY-124308
    PS315

    		PKC Cancer
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-14342
    MK-5046
    1 Publications Verification

    		 Bombesin Receptor Metabolic Disease
    MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity.
  • 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-P1576A
    AMARA peptide TFA

    		AMPK Others
    AMARA peptide (TFA) is a substrate for salt-inducible kinase (SIK) and adenosine monophosphate activated protein kinase (AMPK).
  • HY-N3425
    Kazinol U

    		AMPK Others
    Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.
  • HY-16716
    Basmisanil
    1 Publications Verification

    RG1662; RO5186582

    		 GABA Receptor Neurological Disease
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
  • 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-N0261
    Aurantio-obtusin
    1 Publications Verification

    		 TNF Receptor COX Inflammation/Immunology Cardiovascular Disease
    Aurantio-obtusin is a anthraquinone compound that can be extracted from cassia seed. Aurantio-obtusin has the effects of decreasing blood pressure, decreasing blood lipids and anti-inflammatory.Aurantio-obtusin is an orally active vasodilator. Aurantio-obtusin ameliorates hepatic steatosis through AMPK/ autophagy- and AMPK/TFEB mediated inhibition of lipid accumulation.
  • HY-136093
    Lixumistat hydrochloride

    HL271; IM156 hydrochloride; HL156A hydrochloride

    		 AMPK Cancer Neurological Disease
    Lixumistat (HL271) hydrochloride (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. Lixumistat hydrochloride attenuates aging-associated cognitive impairment in animal model. Lixumistat hydrochloride is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-151385
    VVD-118313

    		JAK STAT IFNAR Interleukin Related Cancer
    VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. VVD-118313 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-128358
    MR-L2

    		Phosphodiesterase (PDE) Neurological Disease
    MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
  • HY-N6971
    Cimiracemoside C

    Cimicifugoside M

    		 AMPK Metabolic Disease
    Cimiracemoside C is an active component of Cimicifuga racemosa, activates AMPK, has the potential activity against diabetes.
  • 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-12755
    ML141
    15+ Cited Publications

    CID-2950007

    		 Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
  • HY-135805
    JBJ-04-125-02

    		EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-136093A
    Lixumistat acetate

    IM156; HL156A; HL271 acetate

    		 AMPK Cancer Neurological Disease
    Lixumistat (IM156; HL156A; HL271) acetate, a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. Lixumistat (acetate) attenuates aging-associated cognitive impairment in animal model. Lixumistat (acetate) is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-103320B
    (1R,2R)-Calhex 231 hydrochloride

    		Others Metabolic Disease
    (1R,2R)-Calhex 231 hydrochloride is the inactive isomer of Calhex 231 hydrochloride (HY-103320A), and can be used as an experimental control. Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • 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-14342A
    (R)-MK-5046

    		Others Metabolic Disease
    (R)-MK-5046 is the inactive isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity.
  • HY-100386
    Ticlopidine

    PCR 5332

    		 Cytochrome P450 Cardiovascular Disease
    Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
  • HY-N2312
    Mogrol
    1 Publications Verification

    		 ERK STAT Cancer
    Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
  • HY-B0923
    Danthron
    1 Publications Verification

    Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone

    		 AMPK Autophagy Bacterial Virus Protease Cancer
    Danthron is a natural product extracted from the traditional Chinese medicine Salvia miltiorrhiza Bunge. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
  • HY-P4910
    Baceridin

    		Proteasome Apoptosis Cancer
    Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research.
  • 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-115570
    GW406108X
    1 Publications Verification

    GW108X

    		 Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
  • 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-16397AS
    Phenformin-d5 hydrochloride

    Phenethylbiguanide-d5 hydrochloride

    		 Isotope-Labeled Compounds Autophagy AMPK Cancer
    Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity[1][2].
  • HY-131958
    D942

    		AMPK Cancer
    D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth.
  • HY-155149
    MAT2A-IN-12

    		Methionine Adenosyltransferase (MAT) Cancer
    MAT2A Allosteric inhibitor 2 is a potent and selective MAT2A allosteric inhibitor with an IC50 of 5 nM. MAT2A Allosteric inhibitor 2 shows nanomolar activity (IC50=5 μM) in the the proliferation assay (MTAP -/- cell line).
  • HY-B1456A
    Fenoprofen

    LILLY-53858

    		 Melanocortin Receptor Inflammation/Immunology
    Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation.
  • 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. BA-53038B has antiviral activity for hepatitis B virus (HBV) with an EC50 value of 3.32 μM. BA-53038B can be used for the research of chronic hepatitis B.
  • HY-134356
    AICA-riboside, 5′-phosphate

    AICAR-5'-MP

    		 Endogenous Metabolite Others
    AICA-riboside, 5′-phosphate (AICAR-5'-MP) is a 5'-phosphorylated analogue of AICAR. AICAR is an adenosine analog and a AMPK activator. .
  • HY-N2447
    Amarogentin
    2 Publications Verification

    		 AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-153886
    Wu-5

    		FLT3 AMPK Apoptosis Cancer
    Wu-5 is a USP10 inhibitor that can inhibit FLT3 and AMPK pathways, induce FLT3-ITD degradation and induce apoptosis.
  • 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-P99171
    Gevokizumab

    		Interleukin Related Inflammation/Immunology
    Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II).
  • HY-115466
    MLT-748
    2 Publications Verification

    		 MALT1 Inflammation/Immunology
    MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM.
  • HY-124587
    MLT-747

    		MALT1 Inflammation/Immunology
    MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 14 nM.
  • HY-125269
    TED-347
    3 Publications Verification

    		 YAP Cancer
    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
  • HY-N4176
    Ginkgolide K

    		Autophagy Neurological Disease
    Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity.
  • HY-13417A
    AICAR phosphate
    110+ Cited Publications

    Acadesine phosphate; AICA Riboside phosphate

    		 AMPK Autophagy YAP Mitophagy Endogenous Metabolite Cancer
    AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
  • HY-136447
    ASP4132
    1 Publications Verification

    		 AMPK Cancer
    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
  • HY-17471A
    Metformin hydrochloride
    95+ Cited Publications

    1,1-Dimethylbiguanide hydrochloride

    		 AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
  • HY-13417
    AICAR
    110+ Cited Publications

    Acadesine; AICA Riboside

    		 AMPK Autophagy YAP Mitophagy Endogenous Metabolite Cancer
    AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
  • HY-N10093
    Chamaejasmine

    Chamaejasmin

    		 Apoptosis AMPK Autophagy Reactive Oxygen Species Cancer
    Chamaejasmine is a biflavonoid that can be isolated from the roots of Stellera chamaejasme L. Chamaejasmine has antitumor activity. Chamaejasmine induces cell apoptosis, autophagy and ROS production, and activates the activity of AMPK/mTOR signal pathway.
  • HY-N1411
    Platycodin D
    4 Publications Verification

    		 AMPK Wnt Metabolic Disease
    Platycodin D is a saponin isolated from Platycodon grandiflorus, acts as an activator of AMPKα, with anti-obesity property. WNT/β-catenin pathway mediates the anti-adipogenic effect of platycodin D.
  • HY-N5083
    Saponarin
    1 Publications Verification

    		 Others Inflammation/Immunology
    Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
  • HY-128770
    LY3154207
    1 Publications Verification

    		 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-112108
    Chitosan oligosaccharide
    4 Publications Verification

    COS

    		 AMPK Endogenous Metabolite Cancer Metabolic Disease
    Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
  • HY-101796
    NSC-70220

    		Others Cancer
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
  • HY-N3005
    Britannin

    		Apoptosis Autophagy Cancer Inflammation/Immunology
    Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
  • HY-N6258
    Kahweol

    		AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-100548
    GSK621
    2 Publications Verification

    		 AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • HY-103269
    BAI1
    4 Publications Verification

    		 Bcl-2 Family Apoptosis Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
  • HY-110228
    Metformin-d6 hydrochloride

    1,1-Dimethylbiguanide-d6 (hydrochloride)

    		 AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
  • HY-B0627
    Metformin
    95+ Cited Publications

    1,1-Dimethylbiguanide

    		 AMPK Autophagy Mitophagy Cancer Metabolic Disease Cardiovascular Disease
    Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy.
  • HY-148189
    Aldometanib
    2 Publications Verification

    LXY-05-029

    		 AMPK Metabolic Disease
    Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.
  • HY-103668A
    SSD114 hydrochloride

    		GABA Receptor Neurological Disease
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
  • HY-100524
    LRE1
    1 Publications Verification

    		 Adenylate Cyclase Cancer
    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  • HY-147421
    Xilmenolone

    		GABA Receptor Neurological Disease
    Xilmenolone is a GABAA receptor positive allosteric modulator.
  • 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-N1419
    Vaccarin

    		AMPK Metabolic Disease
    Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
  • 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-12683
    BPTES
    20+ Cited Publications

    		 Glutaminase Cancer
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
  • HY-59047
    Tolimidone
    3 Publications Verification

    MLR-1023

    		 Src Metabolic Disease
    Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
  • HY-101845
    FITM
    1 Publications Verification

    		 mGluR Cancer
    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  • HY-150079
    HIV-1 integrase inhibitor 10

    		HIV Integrase Infection
    HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
  • 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-18296
    AKT-IN-1
    4 Publications Verification

    		 Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-107507
    Ro 01-6128

    		mGluR Neurological Disease
    Ro 01-6128 is a positive allosteric modulator of mGluR1.
  • HY-110158
    UNC2327

    		Histone Methyltransferase Cancer
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
  • HY-112788
    ONO-8590580

    		GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • HY-N0072
    Brazilin

    		Apoptosis Autophagy Cancer Inflammation/Immunology
    Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities.
  • HY-N2534
    Karanjin

    		AMPK Apoptosis Cancer
    Karanjin is a major active furanoflavonol constituent of Fordia cauliflora. Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.
  • HY-17537
    APY29
    5+ Cited Publications

    		 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-103519
    rac-BHFF

    		GABA Receptor Neurological Disease
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor.
  • HY-139871
    hTrkA-IN-2

    		Others Neurological Disease
    hTrkA-IN-2 is a selective hTrkA allosteric inhibitor with an IC50 value of 3.9 nM.
  • HY-15476
    VU 0364439

    		mGluR Neurological Disease
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
  • HY-142296
    RORγt inhibitor 1

    		ROR Inflammation/Immunology
    RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC50 value of 1 nM.
  • HY-150067
    CB1R antagonist 1

    		Cannabinoid Receptor Metabolic Disease
    CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity.
  • HY-N0735
    Phellodendrine chloride

    		Autophagy Cancer
    Phellodendrine chloride is a plant alkaloid found in Phellodendron amurense. Phellodendrine chloride suppresses the proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis . Phellodendrine chloride promotes autophagy by regulating the AMPK/mTOR pathway and reduce the intestinal damage of ulcerative colitis.
  • HY-142618
    TNF-α-IN-6

    		TNF Receptor Inflammation/Immunology
    TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα (KD = 6.8 nM).
  • HY-153247
    GSK3839919A

    		HIV Integrase Infection Inflammation/Immunology
    GSK3839919A is a potent and allosteric HIV-1integrase inhibitor.
  • HY-116009
    RMC-4550
    3 Publications Verification

    		 SHP2 Phosphatase Cancer
    RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC50 of 0.583 nM.
  • HY-100336
    AC260584

    		mAChR Neurological Disease
    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
  • 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-15857
    CW-069

    		Kinesin Cancer
    CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
  • HY-119208
    VUF11211

    		CXCR Others
    VUF11211 is an allosteric inverse CXCR3 agonist with a Kd of 0.65 nM.
  • HY-142648
    MLT-985

    		MALT1 Cancer
    MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.
  • HY-13449
    TAK-733
    4 Publications Verification

    		 MEK Cancer
    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
  • HY-N3426
    Kazinol B

    		NO Synthase Akt AMPK Metabolic Disease
    Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research.
  • HY-N0592A
    Demethyleneberberine chloride

    		NF-κB AMPK Cancer Infection Metabolic Disease Inflammation/Immunology
    Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD).
  • HY-13418
    Dorsomorphin dihydrochloride
    405+ Cited Publications

    Compound C dihydrochloride; BML-275 dihydrochloride

    		 AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
  • HY-103400
    8-Chloroadenosine

    8-Cl-Ado

    		 AMPK Autophagy Cancer
    8-Chloroadenosine (8-Cl-Ado), a unique ribonucleoside analog, depletes endogenous ATP that subsequently induces the phosphorylation and activation of AMPK. 8-Chloroadenosine induces autophagic cell death. 8-Chloroadenosine effectively inhibited in vivo tumor growth in mice.
  • HY-N0592
    Demethyleneberberine

    		NF-κB AMPK Cancer Infection Metabolic Disease Inflammation/Immunology
    Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
  • HY-14451
    PF-4778574

    		iGluR Neurological Disease
    PF-4778574 is a positive allosteric modulation of AMPA receptor with EC50 of 45 to 919 nM in differenct cells.
  • 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-100519
    NVS-PAK1-1
    1 Publications Verification

    		 PAK Cancer
    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
  • HY-14846A
    Litronesib Racemate

    LY2523355 Racemate

    		 Kinesin Others
    Litronesib Racemate (LY2523355 Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
  • HY-121848
    VU0155094

    ML397

    		 mGluR Neurological Disease
    VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.
  • HY-112094
    WNK-IN-11
    1 Publications Verification

    		 Ser/Thr Protease Others
    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  • HY-120953
    GAT228

    		Cannabinoid Receptor Inflammation/Immunology
    GAT228, the enantiomer of GAT211, is an allosteric cannabinoid receptor 1 (CB1) ligand.
  • HY-141645
    IMM-H007

    WS070117

    		 AMPK TGF-β Receptor NF-κB JNK AP-1 Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
  • HY-133859
    M084

    		Mitochondrial Metabolism Metabolic Disease
    M084 is a benzimidazole derivative. M084 inhibits the mitochondrial respiration, activate mitochondrial unfolded protein response and AMPK, recruites SIR-2.1 and SKN-1, and finally through the transcription factor DAF-16, delays the aging process of C. elegans.
  • HY-134656
    BC1618
    1 Publications Verification

    		 AMPK Mitophagy E1/E2/E3 Enzyme Metabolic Disease Inflammation/Immunology
    BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
  • HY-N6904
    Crocetin monomethyl ester

    		Amyloid-β Inflammation/Immunology Neurological Disease
    Crocetin monomethyl ester, isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity. Crocetin monomethyl ester promotes clearance of amyloid-β by inducing autophagy via the STK11/LKB1-mediated AMPK pathway.
  • HY-70037
    Cinacalcet
    10+ Cited Publications

    AMG 073

    		 CaSR Endogenous Metabolite Cardiovascular Disease Cancer
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.
  • HY-132926
    HPK1-IN-8

    		MAP4K Cancer
    HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
  • HY-156682
    JNT-517

    		Biochemical Assay Reagents Metabolic Disease
    JNT-517 is an oral SLC6A19 allosteric inhibitor for the study of phenylketonuria (PKU).
  • HY-18601
    (±)-BI-D
    5 Publications Verification

    		 HIV HIV Integrase Infection
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
  • HY-15599
    SSR128129E
    1 Publications Verification

    SSR

    		 FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-112247
    SR 16832

    		PPAR Metabolic Disease
    SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites.
  • HY-15713
    NMS-873
    5+ Cited Publications

    		 p97 Cancer
    NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC50 value of 30 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-15252
    Reparixin L-lysine salt
    45+ Cited Publications

    Repertaxin L-lysine salt

    		 CXCR Cancer Inflammation/Immunology Endocrinology
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-N0404
    Sinigrin

    		p38 MAPK AMPK Metabolic Disease Inflammation/Immunology
    Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Sinigrin inhibits early-stage adipogenesis of 3T3-L1 adipocytes through the AMPK and MAPK signaling pathways. Sinigrin has potent anti-oxidant, anti-tumor and anti-inflammatory effects.
  • HY-119137
    AMDE-1

    		Autophagy AMPK Cancer
    AMDE-1 is a potent autophagy inducer. AMDE-1 induces autophagy by the AMPK-mTORC1-ULK1 pathway and at the same time inhibited autophagy-mediated degradation by causing lysosome dysfunction. AMDE-1 can be used in research of cancer.
  • 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-101068
    TOFA
    5+ Cited Publications

    RMI14514; MDL14514

    		 Acetyl-CoA Carboxylase Cancer
    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  • 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-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-70037A
    Cinacalcet hydrochloride
    10+ Cited Publications

    AMG-073 hydrochloride

    		 CaSR Endogenous Metabolite Cardiovascular Disease Cancer
    Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-15599A
    SSR128129E free acid

    SSR free acid

    		 FGFR Cancer
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-147260
    Dalzanemdor

    SAGE-718

    		 iGluR Others
    Dalzanemdor (SAGE-718) is a N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator.
  • HY-114453
    SHP389

    		SHP2 Phosphatase Others
    SHP389 is an allosteric SHP2 inhibitor, with an IC50 of 36 nM for both SHP2 and p-ERK.
  • HY-12408
    6H05

    		Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-W058849
    MT 63-78

    		AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-16397
    Phenformin

    Phenethylbiguanide

    		 Apoptosis AMPK Mitochondrial Metabolism Cancer Metabolic Disease
    Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis.
  • HY-119217
    AZ084
    2 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology
    AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer.
  • HY-141510A
    myo-Inositol trispyrophosphate hexa-triethylamine

    ITPP hexa-triethylamine

    		 Others Others
    myo-Inositol trispyrophosphate (ITPP) hexa-triethylamine, a inositol tripyrophosphate (ITPP) salt, is a membrane permeant allosteric effector of haemoglobin.
  • HY-103535
    GBLD345

    		GABA Receptor Neurological Disease
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM).
  • HY-148788
    Osivelotor

    GBT-601; GBT-021601

    		 Others Others
    Osivelotor is an allosteric modulator of haemoglobin S (HbS). Osivelotor can be used in the study of sickle cell disease (SCD).
  • HY-12408A
    6H05 TFA

    		Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-125880
    SBI-553
    1 Publications Verification

    		 Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-150621
    AS1134900

    		Others Cancer
    AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor.
  • 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-P5860
    MmTx1 toxin

    Micrurotoxin 1

    		 GABA Receptor Neurological Disease
    MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist.
  • 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-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-14419
    TCN238

    		mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • HY-18928
    FAK inhibitor 5

    		FAK Cancer
    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
  • HY-17437A
    Mefloquine hydrochloride
    2 Publications Verification

    Mefloquin hydrochloride

    		 Parasite SARS-CoV Autophagy Potassium Channel ROS Kinase Cancer Infection Metabolic Disease Inflammation/Immunology
    Mefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine hydrochloride is also a K + channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research.
  • 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-15618
    MK-7622

    M1 receptor modulator

    		 mAChR Neurological Disease
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
  • 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 Endogenous Metabolite Neurological Disease
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
  • HY-111446
    EPAC 5376753

    		Ras Cancer Metabolic Disease Cardiovascular Disease
    EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
  • 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-101419
    CYM-5541

    ML249

    		 LPL Receptor Cardiovascular Disease
    CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
  • 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-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-21297
    3,5-Dihydroxy-2-naphthoic acid

    		iGluR Neurological Disease
    3,5-Dihydroxy-2-naphthoic acid is a Naphthoic acid derivative. Naphthoic acid is a NMDA receptor allosteric modulator.
  • HY-14562
    TBPB

    		mAChR Neurological Disease
    TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
  • HY-133556
    IQZ23

    		AMPK Metabolic Disease
    IQZ23 inhibits adipocyte differentiation via AMPK pathway activation. IQZ23 exerts a high efficacy in decreasing the triglyceride level (EC50=0.033 μM) in 3T3-L1 adipocytes. IQZ23 could be used for the research of obesity and related metabolic disorders.
  • HY-126307
    Urolithin B
    2 Publications Verification

    		 NF-κB JNK ERK Akt AMPK Endogenous Metabolite Inflammation/Immunology
    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
  • HY-P2048A
    MOTS-c(human) acetate

    		AMPK GLUT Metabolic Disease
    MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
  • HY-13418A
    Dorsomorphin
    405+ Cited Publications

    Compound C; BML-275

    		 AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
  • 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-B0799
    Dihydroergotoxine mesylate

    Ergoloid mesylates

    		 GABA Receptor Neurological Disease
    Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.
  • HY-15251
    Reparixin
    45+ Cited Publications

    Repertaxin; DF 1681Y

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-50081
    CCR2-RA-[R]
    4 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology
    CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.
  • HY-122913
    Borussertib

    		Akt Cancer
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt.
  • HY-153182
    GBT1118

    		Others Cardiovascular Disease
    GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia.
  • HY-18654
    ADX88178
    1 Publications Verification

    		 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-153306
    RLY-2608

    		PI3K Cancer
    RLY-2608 is a first-in-class allosteric mutant-selective inhibitor of PI3Ka.
  • 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-12446
    K-Ras(G12C) inhibitor 9

    		Ras Cancer
    K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C).
  • HY-138630
    AG-270
    1 Publications Verification

    		 Methionine Adenosyltransferase (MAT) Cancer
    AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.
  • HY-10971A
    Alisertib sodium

    MLN 8237 sodium

    		 Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-13755
    Sulforaphane
    30+ Cited Publications

    		 HDAC Keap1-Nrf2 Apoptosis Cancer Inflammation/Immunology
    Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
  • HY-157166
    EGFR kinase inhibitor 2

    		EGFR Cancer
    EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer.
  • 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-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-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-139641
    PTP1B-IN-14

    		Phosphatase Others
    PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.
  • HY-155036
    Z1078601926

    		Dopamine Transporter Neurological Disease
    Z1078601926 is an allosterical inhibitor of human dopamine transporter (hDAT). Z1078601926 has synergistic effect with Nomifensine (HY-B1110).
  • HY-A0005
    Clofarabine
    3 Publications Verification

    		 Nucleoside Antimetabolite/Analog Autophagy Apoptosis Metabolic Disease Cancer
    Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit.
  • 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-12042
    Pimasertib
    5+ Cited Publications

    AS703026; MSC1936369B

    		 MEK Cancer
    Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
  • HY-114381
    GT 949

    		EAAT Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-112128
    USP7-IN-3

    		Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-103571
    VU0285683

    		mGluR Neurological Disease
    VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety.
  • 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-139640
    PTP1B-IN-13

    		Phosphatase Others
    PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.
  • 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-17601
    Alofanib
    3 Publications Verification

    RPT835

    		 FGFR Apoptosis Cancer Cardiovascular Disease
    Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.
  • HY-155088
    MK-8768

    		mGluR Metabolic Disease
    MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
  • HY-136717
    FBPase-1 inhibitor-1

    		FBPase Metabolic Disease
    FBPase-1 inhibitor-1 (compound 1) is a allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1).
  • 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-135601
    Cinacalcet metabolite M4

    		Drug Metabolite Cardiovascular Disease
    Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease.
  • HY-123617
    AZ8838

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
  • HY-141524
    RMC-3943

    		SHP2 Phosphatase Cancer
    RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC50 = 2.19 nM).
  • HY-15142
    Doxorubicin hydrochloride
    335+ Cited Publications

    Hydroxydaunorubicin hydrochloride

    		 Topoisomerase ADC Cytotoxin AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Cancer Infection
    Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.
  • HY-B2099S
    Buformin-d9 hydrochloride

    1-Butylbiguanide-d9 hydrochloride

    		 Isotope-Labeled Compounds AMPK Cancer Metabolic Disease
    Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
  • HY-10971
    Alisertib
    30+ Cited Publications

    MLN 8237

    		 Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-132806
    Alogabat

    RG-7816; RO-7017773

    		 GABA Receptor Neurological Disease
    Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1).
  • 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-70037S
    Cinacalcet-D3

    AMG 073-d3

    		 CaSR Endogenous Metabolite Cardiovascular Disease
    Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-N0197
    Baicalin
    10+ Cited Publications

    Baicalein 7-O-β-D-glucuronide

    		 NF-κB Autophagy HIV Inflammation/Immunology Cancer
    Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.
  • 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-107841
    K-Ras(G12C) inhibitor 6

    		Ras Cancer
    K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C).
  • HY-13619
    Efaproxiral
    1 Publications Verification

    RSR13

    		 Reactive Oxygen Species Cancer
    Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
  • HY-100667
    UBP608

    		iGluR Neurological Disease
    UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders.
  • 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-111184
    PIK-108

    		PI3K Cancer
    PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
  • 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-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 research of a variety of central nervous system (CNS) disorders.
  • HY-B1221
    Flufenamic acid
    3 Publications Verification

    		 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-N12386
    SIRT1 activator 1

    		Sirtuin Cancer
    SIRT1 activator 1(compound 3) is a derivative of marine compound xyloallenoide A isolated from the mangrove fungus Xylaria sp.SIRT1 activator 1 shows angiogenic activities in zebrafish. SIRT1 activator 1 protects hEPC against AngII-induced senescence by increasing SIRT1 expression levels and balancing the AMPK/Akt signaling pathway.
  • HY-110179
    PSNCBAM-1

    		Cannabinoid Receptor Metabolic Disease
    PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity.
  • HY-19904
    Adomeglivant
    4 Publications Verification

    LY2409021

    		 GCGR Metabolic Disease
    Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.
  • 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-12682
    Glutaminase C-IN-1
    5 Publications Verification

    Compound 968

    		 Glutaminase Cancer
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
  • HY-117408
    VU6004256

    		mAChR Neurological Disease
    VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia.
  • HY-13619A
    Efaproxiral sodium
    1 Publications Verification

    RSR13 sodium

    		 Reactive Oxygen Species Cancer
    Efaproxiral sodium (RSR13 sodium) is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.
  • HY-19519A
    Ladarixin sodium

    DF 2156A

    		 CXCR Infection Inflammation/Immunology
    Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma.
  • 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-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-70037AS
    Cinacalcet-d3 hydrochloride

    AMG 073-d3 (hydrochloride)

    		 CaSR Endogenous Metabolite Cardiovascular Disease
    Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • 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-124137
    Runx1-CBFβ interaction inhibitor 1

    		Others Cancer
    Runx1-CBFβ interaction inhibitor 1 is an allosteric inhibitior of Runt domain-CBFb interaction (IC50=3.2 μM).
  • HY-124372
    JNJ-46356479

    		mGluR Neurological Disease
    JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo.
  • HY-155628
    AMPA receptor modulator-6

    		iGluR Others
    AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases.
  • 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-136311
    NCT-504

    		Others Neurological Disease
    NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
  • HY-18286
    NCGC00229600

    		TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
  • HY-15142A
    Doxorubicin

    Hydroxydaunorubicin

    		 ADC Cytotoxin Antibiotic Bacterial Topoisomerase AMPK HIV Autophagy Mitophagy Apoptosis HBV Cancer Infection
    Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
  • HY-10249
    GSK-690693
    25+ Cited Publications

    		 Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-124896
    Bonannione A

    6-Geranylnaringenin; Mimulone

    		 Phosphatase Apoptosis Autophagy Cancer Inflammation/Immunology
    Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity.
  • HY-114368A
    Kira8 Hydrochloride

    AMG-18 Hydrochloride

    		 IRE1 Inflammation/Immunology
    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • 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

    CAD-9303

    		 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-19519
    Ladarixin

    DF 2156A free base

    		 CXCR Cancer Inflammation/Immunology
    Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma.
  • 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-148799
    Sevasemten

    		Myosin Others
    Sevasemten is an allosteric inhibitor of skeletal muscle myosin. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively.
  • HY-114368
    Kira8
    5+ Cited Publications

    AMG-18

    		 IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-10595
    RO-28-1675
    1 Publications Verification

    		 Glucokinase Metabolic Disease
    RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes.
  • HY-101455
    CDN1163
    5+ Cited Publications

    		 Calcium Channel Metabolic Disease
    CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.
  • HY-146223
    AZD4625

    		Ras Cancer
    AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability.
  • HY-114164
    Thrombin (MW 37kDa)
    4 Publications Verification

    		 Thrombin Neurological Disease
    Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins.
  • 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-110285
    ML382

    		Mas-related G-protein-coupled Receptor (MRGPR) 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-13417S
    AICAR-13C2,15N

    Acadesine-13C2,15N; AICA Riboside-13C2,15N

    		 Isotope-Labeled Compounds Others
    AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N)is the 13C and 15N labeledAICAR(HY-13417). AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
  • HY-124984
    ML353

    		mGluR Neurological Disease
    ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker. ML353 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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-125176
    G907

    		Bacterial Infection
    G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket.
  • 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-104010A
    Asciminib hydrochloride
    4 Publications Verification

    ABL001 hydrochloride

    		 Bcr-Abl Cancer
    Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  • HY-148231
    Dideoxy-amanitin

    		DNA/RNA Synthesis ADC Cytotoxin Cancer
    Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM.
  • HY-104010
    Asciminib
    4 Publications Verification

    ABL001

    		 Bcr-Abl Cancer
    Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  • 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[1][2][3].
  • HY-P1125
    4-CMTB
    2 Publications Verification

    		 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-114304
    COH000
    1 Publications Verification

    		 E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • 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-123269
    PKUMDL-WQ-2101

    		Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    PKUMDL-WQ-2101 is a non-NAD +-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity.
  • 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 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-18652
    Avutometinib
    1 Publications Verification

    Ro 5126766; CH5126766

    		 MEK Raf Cancer
    Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
  • 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-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-10167A
    Tecalcet Hydrochloride
    1 Publications Verification

    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-124646
    KIRA-7

    		IRE1 Inflammation/Immunology
    KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
  • HY-110122
    AZ 12216052

    		mGluR Neurological Disease
    AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.
  • 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-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-151115
    JNJ-1289

    		Others Cancer Inflammation/Immunology
    JNJ-1289 is a potent, selective, competitive and allosteric human spermine oxidase (hSMOX) inhibitor (IC50: 50 nM). JNJ-1289 can be used in the research of polyamine catabolism, inflammation and cancers.
  • HY-153615
    CVN636

    		mGluR Neurological Disease
    CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability.
  • HY-112083
    BAY-3827
    2 Publications Verification

    		 AMPK Cancer
    BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.
  • HY-10299
    GSK-923295
    30+ Cited Publications

    		 Kinesin Apoptosis Cancer
    GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.
  • 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-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-100018
    BAY1125976

    		Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
  • 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-B1221S1
    Flufenamic acid-13C6

    		Isotope-Labeled Compounds 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 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-N0385
    Gomisin J
    3 Publications Verification

    		 AMPK Calcium Channel Metabolic Disease Cardiovascular Disease
    Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease.
  • HY-B1221S
    Flufenamic acid-d4

    		Isotope-Labeled Compounds 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 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-115463
    EB-3D
    1 Publications Verification

    		 AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-18555
    TMPA
    1 Publications Verification

    		 AMPK Cancer Metabolic Disease Inflammation/Immunology
    TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.
  • HY-101071
    (S)-Monastrol

    (+)-Monastrol

    		 Kinesin Cancer
    (S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles.
  • HY-15198
    KG5

    		Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
  • HY-107505
    CBiPES hydrochloride

    		mGluR Neurological Disease
    CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC50: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease.
  • HY-107111
    GSK1034702

    		Cholinesterase (ChE) Neurological Disease
    GSK1034702 is a M1 mAChR allosteric agonist. GSK1034702 shows procognitive effects in rodents. GSK1034702 modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction.
  • HY-135914
    JBJ-02-112-05

    		EGFR Cancer
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFR L858R/T790M.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    		 GABA Receptor Endogenous Metabolite 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-110145
    MRS 1477

    		TRP Channel Cancer
    MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis.
  • 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-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-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-107774
    BMS-986163

    		iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-139202
    XVA143

    		Integrin Inflammation/Immunology
    XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.
  • HY-122150
    AMPA receptor modulator-3

    		iGluR Neurological Disease
    AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC50: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory.
  • HY-15301
    CC0651

    		E1/E2/E3 Enzyme Cancer
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27 Kip1, as confirmed by dose-response analysis.
  • HY-120634
    BMS-929075

    		HCV Infection
    BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity.
  • 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-137067
    IMT1B
    3 Publications Verification

    LDC203974

    		 DNA/RNA Synthesis Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
  • 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-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-110237
    BX430

    		P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
  • HY-151949
    TrkA-IN-4

    		Trk Receptor Neurological Disease
    TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects.
  • 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-15251A
    (Rac)-Reparixin

    (Rac)-Repertaxin; (Rac)-DF 1681Y

    		 Others Cancer Endocrinology Inflammation/Immunology
    (Rac)-Reparixin is the inactive isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-112209
    VU0467154
    1 Publications Verification

    		 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-117571
    Zatolmilast
    1 Publications Verification

    BPN14770

    		 Phosphodiesterase (PDE) Neurological Disease
    Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, 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-119377
    UPGL00004

    		Glutaminase Cancer
    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  • HY-145684
    EP2 receptor antagonist-1

    		Prostaglandin Receptor Inflammation/Immunology
    EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects.
  • 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-13848
    AZD8797
    10+ Cited Publications

    KAND567

    		 CX3CR1 CXCR Inflammation/Immunology Endocrinology
    AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
  • 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-N0930B
    Galegine hydrochloride

    		AMPK Bacterial Infection Metabolic Disease
    Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.
  • HY-139058
    23-epi-26-Deoxyactein

    27-Deoxyactein

    		 PPAR Cancer Metabolic Disease
    23-epi-26-Deoxyactein is a natural and orally active anti-obesity and anti-cancer compound.
  • HY-50683
    JNJ-38877605
    3 Publications Verification

    		 c-Met/HGFR Cancer Metabolic Disease
    JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach.
  • HY-121726
    3HOI-BA-01

    		Autophagy mTOR Cardiovascular Disease
    3HOI-BA-01 is amTORinhibitor.3HOI-BA-01reduces infarct size and inducedautophagyin a murine myocardial ischemia/reperfusion injury model.
  • HY-N4100
    Trilobatin
    1 Publications Verification

    		 HIV SGLT Infection
    Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
  • HY-13058
    ADX-47273
    1 Publications Verification

    		 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-116819A
    VU0453379 hydrochloride

    		GCGR Metabolic Disease
    VU0453379 hydrochloride 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-150018
    N-Demethyl MK-6884

    		mAChR Neurological Disease
    N-Demethyl MK-6884 (compound 34) is a potent M4 mAChR allosteric modulator. N-Demethyl MK-6884 can be used in the studies of alzheimer's disease and other diseases mediated by the M4 mAChR.
  • HY-50862
    Akt1/Akt2-IN-1

    		Akt Cancer
    Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-110124
    ML202

    		Pyruvate Kinase Cancer
    ML202 is a highly specific allosteric activator of human pyruvate kinase M2 (hPK-M2), which can affect the cooperativity of phosphoenolpyruvate (PEP) binding, while adenosine diphosphate (ADP) binding almost no effect.
  • 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-70074
    CCG-63802
    1 Publications Verification

    		 RGS Protein Cancer Inflammation/Immunology
    CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM.
  • HY-156681
    STX-478

    		PI3K Cancer
    STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research.
  • HY-120004
    PF-06827443

    		mAChR Infection
    PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion.
  • 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-13831
    BPTU

    BMS-646786

    		 P2Y Receptor Cancer Neurological Disease
    BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.
  • HY-16926
    CK-666
    4 Publications Verification

    		 Arp2/3 Complex HIV Cancer Infection
    CK-666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC50=12 μM). CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.
  • HY-112942
    CMP-Sialic acid

    CMP-Neu5Ac

    		 Endogenous Metabolite Metabolic Disease
    CMP-Sialic acid (CMP-Neu5Ac) is an allosteric inhibitor of UDP-GlcNAc 2-epimerase. CMP-Sialic acid provides a substrate for Golgi sialyltransferases. CMP-Sialic acid is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates.
  • HY-10519
    BMS-345541
    15+ Cited Publications

    		 IKK Cancer
    BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
  • HY-10933S
    CX516-d10

    BDP 12-d10

    		 Isotope-Labeled Compounds iGluR Neurological Disease
    CX516-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)[1].
  • HY-13619S
    Efaproxiral-d6

    		Reactive Oxygen Species Cancer
    Efaproxiral-d6 is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
  • 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-10518
    BMS-345541 hydrochloride
    15+ Cited Publications

    		 IKK Cancer
    BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
  • HY-112942A
    CMP-Sialic acid sodium salt

    CMP-Neu5Ac sodium salt

    		 Endogenous Metabolite Metabolic Disease
    CMP-Sialic acid (CMP-Neu5Ac) sodium salt is an allosteric inhibitor of UDP-GlcNAc 2-epimerase. CMP-Sialic acid sodium salt provides a substrate for Golgi sialyltransferases. CMP-Sialic acid sodium salt is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates.
  • HY-W011102
    S-Trityl-L-cysteine

    NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine

    		 Kinesin Apoptosis Cancer
    S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities.
  • HY-10219
    Rapamycin
    Maximum Cited Publications
    677 Publications Verification

    Sirolimus; AY-22989

    		 mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • 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-154848
    UCL-TRO-1938

    		PI3K Cancer
    UCL-TRO-1938 is a potent allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects.
  • HY-143312A
    V-0219 hydrochloride

    		GLP Receptor Metabolic Disease
    V-0219 hydrochloride (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 hydrochloride can be used for obesity-associated diabetes research.
  • 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-10358
    MK-2206 dihydrochloride
    265+ Cited Publications

    MK-2206 (2HCl)

    		 Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-10355
    AKT inhibitor VIII
    35+ Cited Publications

    AKTi-1/2

    		 Akt Apoptosis Cancer Metabolic Disease
    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
  • HY-12429
    Beclabuvir
    3 Publications Verification

    BMS-791325

    		 HCV Infection
    Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM. 
  • HY-18370
    HIF-2α-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
  • HY-156659
    NC1

    		Phosphatase Others
    NC1 is a noncompetitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 inhibits LYP by restricting the movement of the WPD-loop. NC1 inhibits LYP-mediated TCR signaling in T cells.
  • HY-112606
    ML-290

    		Others Others
    ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM. ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
  • HY-100405
    FTIDC

    		mGluR Neurological Disease
    FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
  • HY-147696
    SMTIN-T140

    		HSP AMPK Reactive Oxygen Species Cancer
    SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells.
  • HY-19843
    MK-0941

    		Glucokinase Metabolic Disease
    MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
  • HY-151948
    TrkA-IN-3

    		Trk Receptor Neurological Disease
    TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC50 of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain.
  • 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-103040
    Zuranolone
    1 Publications Verification

    SAGE-217; BIIB125

    		 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-156331
    VU6004909

    		mGluR Neurological Disease
    VU6004909 is a mGlu5 receptor positive allosteric modulator (pEC50: 7.59). VU6004909 shows antipsychotic-like effects. VU6004909 can reverse MK801-induced cortical hyperactivity and cognitive deficits.
  • HY-10198
    Navarixin
    15+ Cited Publications

    SCH 527123; MK-7123

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
  • 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-15756
    PTP1B-IN-4

    		Phosphatase Metabolic Disease
    PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes.
  • HY-12316
    20(S)-Hydroxycholesterol
    1 Publications Verification

    20α-Hydroxycholesterol

    		 Smo Endogenous Metabolite Cancer
    20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
  • HY-119751
    Hematein

    		Casein Kinase Akt Wnt Apoptosis Cancer
    Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
  • HY-156634
    Risevistinel

    NYX-783

    		 iGluR Neurological Disease
    Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
  • HY-155810
    DQP-26

    		iGluR Neurological Disease
    DQP-26 is a potent NMDAR negative allosteric modulator with IC50 values of 0.77 μM and 0.44 μM for GluN2C and GluN2D, respectively. DQP-26 has the potential for NMDAR-associated neurological disease research.
  • HY-10250
    Triciribine phosphate

    TCN-P

    		 ATP Synthase Metabolic Disease
    Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits  IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity.
  • HY-113320S
    Etiocholanolone-d5

    		GABA Receptor Endogenous Metabolite Neurological Disease
    Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
  • 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-114334
    Glutaminase-IN-1

    CB839 derivative

    		 Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • 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-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-100214
    EAI001

    		EGFR Cancer
    EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer.
  • HY-W009731
    Dibenzoylmethane

    		Keap1-Nrf2 Cancer Metabolic Disease
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
  • HY-15831
    L-838417-d9

    		Isotope-Labeled Compounds GABA Receptor Neurological Disease
    L-838417-d9 is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].
  • HY-15446
    Basimglurant
    1 Publications Verification

    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. Basimglurant is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-16579
    Etifoxine hydrochloride
    1 Publications Verification

    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-133862
    SCH-202676

    		Influenza Virus G protein-coupled Bile Acid Receptor 1 Adenosine Receptor Infection
    SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 µM.
  • 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-141510
    myo-Inositol trispyrophosphate hexasodium

    ITPP hexasodium

    		 Others Cancer
    myo-Inositol trispyrophosphate (ITPP) hexasodium, a modifier of haemoglobin, is an allosteric effector that reduces the oxygen‐binding affinity of haemoglobin and facilitates the release of oxygen by red blood cells. myo-Inositol trispyrophosphate can reverse hypoxia, control tumor growth and improve chemotherapy response.
  • HY-153193
    LSN3160440

    		GLP Receptor Molecular Glues Metabolic Disease
    LSN3160440 is an allosteric modulator of GLP-1R, which acts as a protein–protein interaction (PPI) stabilizer or molecular glue to assist in the adhesion of inactive GLP-1 (9-36) NH2 on GLP-1R.
  • HY-130297
    PROTAC BCR-ABL1 ligand 1

    		Bcr-Abl Cancer
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
  • 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[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
  • HY-16579A
    Etifoxine
    1 Publications Verification

    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-103528
    SCS

    Salicylidene salicylhydrazide

    		 GABA Receptor Inflammation/Immunology Neurological Disease
    SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.
  • HY-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    		 mTOR FKBP Autophagy Cancer
    Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
  • HY-141848A
    (S,S)-BMS-984923

    		mGluR Neurological Disease
    (S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor. BMS-984923 is a potent mGluR5 silent allosteric modulator.
  • 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-131902
    MLT-231

    		MALT1 Cancer
    MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
  • 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-136128
    H3B-120

    		Potassium Channel Cancer
    H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
  • 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-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-149241
    SHP2-IN-13

    		SHP2 Cancer
    SHP2-IN-13 is a highly selective and orally active SHP2 “tunnel site” allosteric inhibitor with an IC50 of 83.0 nM. SHP2-IN-13 has the potential for cancers bearing RTK oncogenic drivers and SHP2-related diseases research.
  • HY-19996
    AH-7614

    		Free Fatty Acid Receptor Metabolic Disease
    AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
  • HY-108668
    TC-P 262

    		P2X Receptor Others
    TC-P 262 is a potent P2X3 inhibitor. TC-P 262 shows inhibition by bindings to hP2X3. TC-P 262 has the potential for the research of rheumatoid arthritis, cough, and pain.
  • HY-114548
    Ebselen oxide

    		Guanylate Cyclase Infection
    Ebselen oxide, the selenone analogue of Ebselen, covalently modifies diguanylate cyclase (DGC) to inhibit c-di-GMP-receptor interactions and reduces DGC activity. Ebselen oxide also inhibits alginate production (IC50=14 μM) by Pseudomonas aeruginosa. Ebselen oxide inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9 (IC50 ranging from 0.2 to 4.7 μM).
  • HY-107509
    LY2389575 hydrochloride

    		mGluR Neurological Disease
    LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
  • HY-113616A
    VU0364572 TFA

    		mAChR Neurological Disease
    VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant.
  • HY-156626
    Nevadistinel

    NYX-458; NYX-3054

    		 iGluR Neurological Disease
    Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
  • HY-152207
    LWG-301

    		Glutaminase Apoptosis Cancer
    LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model.
  • HY-110012
    SCH-202676 hydrobromide

    		Infection
    SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM.
  • HY-155026
    UPCDC30766

    		p97 Cancer
    UPCDC30766 is a potent allosteric inhibitor of p97, with an IC50 of 12 nM. UPCDC30766 can be used for the research of colon cancer. UPCDC30766 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-103423
    PAOPA

    		Dopamine Receptor Neurological Disease
    PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists.
  • HY-10046
    Plerixafor
    55+ Cited Publications

    AMD 3100; JM3100; SID791

    		 CXCR HIV Cancer Infection Endocrinology Inflammation/Immunology
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • 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-113050
    2,3-Diphosphoglyceric acid

    2,3-DPG

    		 Others Others
    2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2,3-Diphosphoglyceric acid binds to hemoglobin and decrease its affinity for oxygen.
  • 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-107651
    VU 0365114

    		mAChR Metabolic Disease
    VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells.
  • HY-149602
    Glutaminase C-IN-2

    		Glutaminase Reactive Oxygen Species Cancer
    Glutaminase C-IN-2 (compound 11) is glutaminase C (GAC) allosteric inhibitor with an IC50 of 10.64 nM. Glutaminase C-IN-2 regulates the cellular metabolite, thereby increasing reactive oxygen species (ROS) by blocking glutamine metabolism. Glutaminase C-IN-2 has anticancer effects.
  • HY-133512
    NCGC00249987

    		Phosphatase Cancer
    NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells.
  • HY-14412
    p38α inhibitor 4

    		p38 MAPK Cancer
    p38α inhibitor 4 (compound 10) is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM. p38α inhibitor 4 exhibits no activity against p38β, p38γ, and p38δ.
  • HY-107588
    TC-I 15

    		Integrin Cardiovascular Disease
    TC-I 15 (TC-I-15) is an allosteric, collagen-binding integrin α2β1 inhibitor with IC50 values of 26.8 μM and 0.4 μM for GFOGER and GLOGEN, respectively. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition.
  • HY-100206
    5α-Androstane-3β,5,6β-triol

    		AMPK Neurological Disease
    5α-Androstane-3β,5,6β-triol is a neuroprotectant. 5α-Androstane-3β,5,6β-triol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. 5α-Androstane-3β,5,6β-triol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo.
  • HY-12062
    PD318088
    1 Publications Verification

    		 MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research.
  • 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-155533
    YF704

    		SHP2 Cancer
    YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells.
  • 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-103575
    MFZ 10-7

    		mGluR Neurological Disease
    MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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-13965
    Parmodulin 2
    2 Publications Verification

    ML161

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-155672
    JPC0323

    		5-HT Receptor Neurological Disease
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease.
  • HY-50688
    SB-265610
    2 Publications Verification

    		 CXCR Inflammation/Immunology
    SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.
  • HY-156757
    MDL-811

    		Sirtuin Cancer
    MDL-811, an allosteric SIRT6 activator, significantly activates SIRT6 histone H3 deacetylation (H3K9Ac, H3K18Ac, and H3K56Ac). MDL-811 could be used in the study of colorectal cancer.
  • HY-134494
    MS48107

    		GPR68 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-144742
    NS2B/NS3-IN-6

    		Virus Protease Infection
    NS2B/NS3-IN-6 (Compound 1a) is an allosteric DENV and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 2.23 µM and 25.2 µM against ZIKV and DENV proteases, respectively.
  • 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-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-122647
    Valiglurax

    VU0652957; VU2957

    		 mGluR Neurological Disease
    Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.
  • HY-P10010
    DB21, Galectin-1 Antagonist

    		Galectin Cancer
    DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models.
  • 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-127111
    NDI-091143
    2 Publications Verification

    		 ATP Citrate Lyase Cancer
    NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate.
  • 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-B0520A
    Benztropine mesylate
    4 Publications Verification

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    		 Dopamine Receptor mAChR Histamine Receptor Cancer Neurological Disease
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
  • HY-151899
    A3AR modulator 1

    		Adenosine Receptor Inflammation/Immunology
    A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax.
  • HY-12689
    Mitapivat

    AG-348

    		 Pyruvate Kinase Metabolic Disease
    Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.
  • 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[1][2][3].
  • 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-113050A
    2,3-Diphosphoglyceric acid pentasodium

    2,3-DPG pentasodium

    		 Others Others
    2,3-Diphosphoglyceric acid (2,3-DPG) pentasodium is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid pentasodium stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2,3-Diphosphoglyceric acid pentasodium binds to hemoglobin and decrease its affinity for oxygen.
  • HY-150186
    RXFP2 agonist 2

    		Others Metabolic Disease
    RXFP2 agonist 2 is a selective，orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis.
  • HY-103524
    Valerenic acid
    1 Publications Verification

    (-)-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-N2597
    Prunetin

    		Aldehyde Dehydrogenase (ALDH) Inflammation/Immunology
    Prunetin, an O-methylated isoflavone, possesses anti-inflammatory activity. Prunetin is a potent human aldehyde dehydrogenases inhibitor.
  • 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-129119
    Akt1/Akt2-IN-2

    		Akt Caspase Cancer
    Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells.
  • HY-B0520
    Benztropine

    Benzatropine; Benzotropine

    		 Dopamine Receptor mAChR Histamine Receptor
    Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
  • HY-N0240
    Herbacetin
    4 Publications Verification

    		 Others Cancer
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
  • HY-101478
    Fenobam

    		mGluR Neurological Disease
    Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
  • HY-115864
    Osavampator

    TAK-653

    		 iGluR Lipoxygenase Neurological Disease
    Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.
  • HY-100939
    4-Chlorophenylguanidine hydrochloride

    		Sodium Channel Neurological Disease
    4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo.
  • HY-108708
    GeA-69

    		PARP Cancer
    GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd value of 2.1 µM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage.
  • 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-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-13340
    VU0152100

    VU152100

    		 mAChR Neurological Disease
    VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.
  • HY-117282
    JG-98
    5 Publications Verification

    		 HSP Apoptosis Cancer
    JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
  • HY-100213
    EAI045
    1 Publications Verification

    		 EGFR Cancer
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
  • HY-102071
    KIN59

    5'-O-Tritylinosine; 5'-O-Trityl-inosine

    		 Nucleoside Antimetabolite/Analog Cancer
    KIN59 (5’-O-Tritylinosine) is a potent thymidine phosphorylase allosteric inhibitor. KIN59 inhibits FGF2-stimulated cell growth. KIN59 inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimulated cells. KIN59 shows anti-tumor activity.
  • 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-17437
    Mefloquine

    Mefloquin

    		 Parasite Autophagy SARS-CoV Potassium Channel ROS Kinase Cancer Infection Metabolic Disease Inflammation/Immunology
    Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K + channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.
  • HY-12687
    Tizoxanide
    5+ Cited Publications

    TIZ

    		 Bacterial HIV Autophagy Parasite IKK Influenza Virus Cancer Infection
    Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.
  • HY-137092
    IACS-13909

    		SHP2 Phosphatase Cancer
    IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
  • HY-107663
    MIF-1

    Pro-Leu-Gly-NH2; Melanostatin

    		 Dopamine Receptor Neurological Disease
    MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
  • HY-113604
    Pentabromopseudilin

    		TGF-β Receptor Cancer
    Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and 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. Dipraglurant is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-149607
    SHP2-IN-22

    		SHP2 Cancer
    SHP2-IN-22 is SHP2 allosteric inhibitor with an IC50 value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research.
  • HY-143312B
    (R)-V-0219

    		GLP Receptor Metabolic Disease
    (R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R.
  • HY-148016
    I-287

    		Protease Activated Receptor (PAR) ERK Inflammation/Immunology
    I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.
  • 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-126327A
    UNC4976 TFA

    		Histone Methyltransferase Cancer
    UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-115452
    G5-7

    		JAK Apoptosis Cancer
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
  • HY-112603A
    AP5 sodium

    		Free Fatty Acid Receptor Metabolic Disease
    AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research.
  • HY-16062
    ARQ 621

    		Kinesin Cancer
    ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor. ARQ 621 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-10046S
    Plerixafor-d4

    		CXCR HIV Cancer Infection Endocrinology Inflammation/Immunology
    Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
  • HY-G0021
    N-Desmethylclozapine

    Norclozapine; Desmethylclozapine; Normethylclozapine

    		 mAChR Opioid Receptor Drug Metabolite Virus Protease Infection
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
  • HY-112603
    AP5

    		Free Fatty Acid Receptor Metabolic Disease
    AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.
  • 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-143312D
    (R)-V-0219 hydrochloride

    		GLP Receptor Metabolic Disease
    (R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R.
  • HY-130608
    Mutated EGFR-IN-3

    		EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • 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-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-123801
    MIDD0301

    GL-II-93

    		 GABA Receptor Others
    MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases.
  • HY-11048
    NS11394
    3 Publications Verification

    		 GABA Receptor Neurological Disease
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
  • HY-15470
    GW791343 trihydrochloride

    		P2X Receptor Neurological Disease
    GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.
  • HY-110190
    VU0422288

    ML396

    		 mGluR Neurological Disease
    VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.
  • HY-B1456AS
    Fenoprofen-13C6(sodium salt hydrate)

    		Isotope-Labeled Compounds Melanocortin Receptor Inflammation/Immunology
    Fenoprofen- 13C6 (sodium hydrate) is the 13C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].
  • 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-15445
    CTEP
    2 Publications Verification

    RO 4956371; mGluR5 inhibitor

    		 mGluR Neurological Disease
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of?mGlu5?receptor with?IC50?of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-15469
    GW791343 dihydrochloride

    		P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
  • HY-147007
    β-catenin-IN-3

    		β-catenin Wnt Cancer
    β-catenin-IN-3 (compound C2) is a potent and selective β-catenin inhibitor with a KD value of 54.96 nM. β-catenin-IN-3 acts by targeting a cryptic allosteric modulation site of β-catenin. β-catenin-IN-3 can significantly reduce viability of β-catenin-driven cancer cells.
  • 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-134177
    2,5-Anhydro-D-glucitol-1,6-diphosphate

    		Pyruvate Kinase Metabolic Disease
    2,5-Anhydro-D-glucitol-1,6-diphosphate is a limited stimulator of yeast Pyruvate Kinase. 2,5-Anhydro-D-glucitol-1,6-diphosphate is used as an analogue of the a-form, 2,5-anhydro-D-mannitol 1,6-bisphosphate, while is an excellent allosteric activator of Pyruvate Kinase.
  • 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-146223A
    (3R,10R,14aS)-AZD4625

    		Others Cancer
    (3R,10R,14aS)-AZD4625 is the inactive isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability.
  • HY-N0226
    Epiberberine

    		Cholinesterase (ChE) Beta-secretase Metabolic Disease Neurological Disease
    Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.
  • HY-N0281
    Daphnetin
    2 Publications Verification

    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-N0226A
    Epiberberine chloride
    2 Publications Verification

    		 Cholinesterase (ChE) Beta-secretase Reactive Oxygen Species Metabolic Disease Neurological Disease
    Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
  • HY-154958
    mTOR inhibitor-12

    		mTOR Neurological Disease
    mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases.
  • HY-A0009
    Galanthamine hydrobromide
    10+ Cited Publications

    Galantamine hydrobromide

    		 Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-144740
    NS2B/NS3-IN-5

    		Virus Protease Infection
    NS2B/NS3-IN-5 (Compound 25b) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.67 µM and 4.38 µM against ZIKV and DENV2 NS2B/NS3 proteases, respectively.
  • HY-144396
    SHP2-IN-8

    		SHP2 Phosphatase Akt Apoptosis Cancer
    SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells.
  • HY-150080
    GSK3739936

    BMS-986180

    		 HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.
  • HY-124634
    PZ-2891
    1 Publications Verification

    		 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-13856
    (R)-PS210

    		PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-131043
    NVS-PAK1-C

    		PAK Cancer
    NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM).
  • HY-148867
    UCM-1306

    2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl

    		 Dopamine Receptor Neurological Disease
    UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
  • HY-P5839
    α-Conotoxin MrIC

    		nAChR Neurological Disease
    α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR.
  • HY-144736
    NS2B/NS3-IN-4

    		Virus Protease Infection
    NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively.
  • HY-128439
    BT173

    		DYRK Cancer
    BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway.
  • HY-107663A
    MIF-1 TFA

    Pro-Leu-Gly-NH2 TFA; Melanostatin TFA

    		 Dopamine Receptor Neurological Disease
    MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
  • 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. VU0360172 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-114169
    WRG-28

    		Discoidin Domain Receptor Cancer Inflammation/Immunology
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice.
  • HY-B0520AS1
    Benztropine-d3 mesylate

    		Dopamine Receptor Histamine Receptor mAChR
    Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
  • HY-120327
    KY-226

    		Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-108232
    MK-2206

    		Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities.
  • 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-P1259
    PR-39

    		Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-19752A
    VU0357017 hydrochloride

    CID-25010775

    		 mAChR Neurological Disease
    VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
  • HY-49444
    EN450

    		E1/E2/E3 Enzyme NF-κB Cancer
    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
  • HY-B0520AS
    Benztropine-13C,d3 mesylate

    		Isotope-Labeled Compounds Dopamine Receptor mAChR Histamine Receptor Cancer Neurological Disease
    Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
  • HY-123636
    UPCDC-30245

    		p97 Cancer
    UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A. UPCDC-30245 can be used in the research of cancer.
  • HY-123418
    PKUMDL-WQ-2201

    		Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth.
  • HY-P1259A
    PR-39 TFA

    		Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-144766
    ATX inhibitor 13

    		Apoptosis Cancer
    ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.
  • 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-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-G0021S
    N-Desmethylclozapine-d8

    Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8

    		 mAChR Opioid Receptor Drug Metabolite Virus Protease Infection
    N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
  • HY-G0021S1
    N-Desmethylclozapine-d8 hydrochloride

    Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride

    		 mAChR Opioid Receptor Drug Metabolite Virus Protease Infection
    N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
  • HY-115627
    PKUMDL-LC-101-D04
    1 Publications Verification

    GPX4-Activator-1d4

    		 Glutathione Peroxidase Inflammation/Immunology
    PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potent ferroptosis regulator glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 increases GPX4 activity to 150% at 20 μM in the cell-free assay and 61 μM in cell extracts.
  • HY-10118
    Filibuvir
    2 Publications Verification

    		 HCV DNA/RNA Synthesis Infection
    Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
  • 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. LSN2463359 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-100403
    Ro 67-7476
    4 Publications Verification

    		 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-123872
    MSC1094308

    		p97 Cancer
    MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively. MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer.
  • HY-122630
    TH-257

    		LIM Kinase (LIMK) Cancer
    TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
  • HY-149975
    AMPA receptor modulator-4

    		iGluR Neurological Disease
    AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice.
  • HY-122247
    PVZB1194

    		Kinesin Cancer
    PVZB1194 is a biphenyl-type inhibitor of Kinesin spindle protein Eg5 or KIF11. Eg5 is related to the cell cycle, and Eg5 inhibition can lead to cell cycle arrest and apoptosis. PVZB1194 exhibits anticancer potential via inhibiting Eg5 ATPase activity. PVZB1194 binds to the α4/α6 allosteric pocket, and shows ATP competetive activity.
  • HY-10357
    MK-2206 free base

    		Akt Autophagy Apoptosis Cancer
    MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities.
  • HY-13509
    CCG-50014
    1 Publications Verification

    		 RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-143312C
    (S)-V-0219

    		GLP Receptor Metabolic Disease
    (S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice.
  • HY-A0009S
    Galanthamine-d3 hydrobromide

    Galantamine-d3 hydrobromide

    		 Isotope-Labeled Compounds Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
  • 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-P4160
    PDC31

    THG113.31; ILGHXDYK

    		 Prostaglandin Receptor Endocrinology
    PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells.
  • HY-P1045
    187-1, N-WASP inhibitor
    1 Publications Verification

    		 Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-151464
    SHP2/HDAC-IN-1

    		SHP2 Phosphatase HDAC Cancer Inflammation/Immunology
    SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.
  • HY-143312E
    (S)-V-0219 hydrochloride

    		GLP Receptor Metabolic Disease
    (S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice.
  • HY-131445A
    SS-RJW100

    		Others Metabolic Disease Inflammation/Immunology
    SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    		Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-151829
    Fmoc-L-Asn(EDA-N3)-OH

    		ADC Linker Others
    Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II.
  • HY-146725
    FBPase-IN-1

    		FBPase Metabolic Disease
    FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase.
  • 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-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-P0172A
    ATI-2341 TFA
    2 Publications Verification

    		 CXCR Cancer Inflammation/Immunology Endocrinology
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-130344
    SKF 83959
    1 Publications Verification

    		 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-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-10219S1
    Rapamycin-13C,d3

    Sirolimus-13C,d3; AY-22989-13C,d3

    		 Isotope-Labeled Compounds Others
    Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-19719A
    Miransertib hydrochloride
    5+ Cited Publications

    ARQ-092 hydrochloride

    		 Akt Parasite Cancer Infection
    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.
  • HY-137458A
    Vevorisertib trihydrochloride

    ARQ 751 trihydrochloride

    		 Akt Cancer
    Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer.
  • HY-19719
    Miransertib
    5+ Cited Publications

    ARQ-092

    		 Akt Parasite Cancer Infection
    Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.
  • HY-P0172
    ATI-2341

    		CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • 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-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-110208
    BRD9876

    		Kinesin Microtubule/Tubulin Cancer
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
  • HY-156025
    HCAR2 agonist 1

    		Others Inflammation/Immunology
    HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis.
  • HY-117163
    FzM1.8

    		Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1
    5+ Cited Publications

    		 Epigenetic Reader Domain Cancer
    BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
  • HY-117287
    Deucravacitinib
    10+ Cited Publications

    BMS-986165

    		 JAK Interleukin Related IFNAR Inflammation/Immunology
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis.
  • HY-153094
    BDM-2

    		HIV HIV Integrase Infection
    BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity.
  • HY-150025
    (4aS,8aR)-NPD-001

    		DNA Methyltransferase Apoptosis Cancer
    (4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882.
  • HY-12545
    Brevetoxin-3

    PbTx-3

    		 Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-100386S
    Ticlopidine-d4

    PCR 5332-d4

    		 Isotope-Labeled Compounds Cytochrome P450 Cardiovascular Disease
    Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
  • HY-156466
    QL-1200186

    		JAK Inflammation/Immunology
    QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice.
  • HY-112289
    IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
  • 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-134539
    IMT1
    3 Publications Verification

    		 Mitochondrial Metabolism DNA/RNA Synthesis Cancer Metabolic Disease
    IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases.
  • 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-124832
    δ-Secretase inhibitor 11

    		Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.
  • HY-112289B
    (1R)-IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    (1R)-IDH889 is the inactive isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
  • HY-15310
    Ivermectin
    15+ Cited Publications

    MK-933

    		 Flavivirus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • 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-122575
    Aurintricarboxylic acid
    1 Publications Verification

    		 P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
  • HY-147183
    JBJ-09-063

    		EGFR Cancer
    JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.
  • 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-147183A
    JBJ-09-063 TFA

    		EGFR Cancer
    JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.
  • HY-147183B
    JBJ-09-063 hydrochloride

    		EGFR Cancer
    JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer.
  • 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.
  • HY-149359
    IHMT-IDH1-053

    		Isocitrate Dehydrogenase (IDH) Cancer
    IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants.