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Targets Recommended: PKA

Results for "Allosteric pka Inhibitors" in MCE Product Catalog:

343

Inhibitors & Agonists

2

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

22

Peptides

21

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-P1290
    PKA Inhibitor Fragment (6-22) amide

    PKI-(6-22)-amide

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-P1290A
    PKA Inhibitor Fragment (6-22) amide TFA

    PKI-(6-22)-amide TFA

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-11007
    GNF-2

    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-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-14691
    Refametinib

    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-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-105858
    BNC210

    H-Ile-Trp-OH; IW-2143

    nAChR Neurological Disease
    BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
  • HY-109128
    Danicamtiv

    Myosin Cancer
    Danicamtiv, an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
  • HY-114397
    SHP394

    Phosphatase Cancer
    SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.
  • 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-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-12306
    8-Bromo-cAMP sodium salt

    8-Br-Camp sodium salt

    PKA Cancer
    8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
  • 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, and is centrally penetrant.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-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-106199
    Adenosine A1 receptor activator T62

    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-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-119339
    SX-682

    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-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-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-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-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-P0248
    Kemptide

    PKA Metabolic Disease
    Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
  • HY-136173
    TNO155

    Phosphatase Cancer
    TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • HY-133073
    CCR7 Ligand 1

    CCR7-Cmp2105

    CCR Ligand 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-P1595
    CREBtide

    PKA Metabolic Disease
    CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA substrate.
  • 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-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-113252
    2-Methoxyestrone

    Endogenous Metabolite Metabolic Disease
    2-Methoxyestrone is a methoxylated catechol estrogen and metabolite of estrone, with a pKa of 10.81.
  • 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

    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-100521
    GKI-1

    Others Cancer
    GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWL FL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA.
  • HY-124308
    PS315

    PKC Cancer
    PS315, a derivative of PS48, 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 PKCι (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-P0291
    Kemptide Phospho-Ser5

    PKA Others
    Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
  • 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-103076
    EZ-482

    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-15979A
    H-89 dihydrochloride

    Protein kinase inhibitor H-89 dihydrochloride

    PKA Autophagy Others
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
  • HY-B1898
    Metadoxine

    PKA Metabolic Disease
    Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
  • HY-P1597
    Malantide

    PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
  • 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-135676
    DHODH-IN-12

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.07.
  • HY-135675
    DHODH-IN-11

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03.
  • HY-N6789
    KT5720

    PKA Bacterial Antibiotic Infection Endocrinology Metabolic Disease
    KT5720 is a cell-permeable, potent, specific, reversible, ATP-competitive inhibitor of protein kinase A (PKA), with a Ki of 60 nM.
  • HY-12755
    ML141

    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-119695A
    Simvastatin acid ammonium

    Tenivastatin ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-P1597A
    Malantide TFA

    PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
  • 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-15292A
    S107 hydrochloride

    Others Cardiovascular Disease
    S107 hydrochloride is a RyR-selective 1,4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-12062
    PD318088

    MEK Cancer
    PD318088 is an allosteric MEK inhibitor.
  • 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-125269
    TED-347

    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-P1291
    PKI 14-22 amide,myristoylated

    PKA Cancer
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-115466
    MLT-748

    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-100984
    HA-100

    PKA PKC Myosin Cancer
    HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50s of 4, 8, 12 and 240 μM, respectively.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-P1291A
    PKI 14-22 amide,myristoylated TFA

    PKA Cancer
    PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-12659
    LX7101

    ROCK Others
    LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.
  • HY-103668A
    SSD114 hydrochloride

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

    Adenylate Cyclase Cancer
    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  • HY-101216
    Org-26576

    iGluR Neurological Disease
    Org-26576 is a AMPA receptor positive allosteric modulator.
  • HY-16423
    Rapacuronium bromide

    Org 9487

    mAChR Neurological Disease
    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  • HY-14612
    CPPHA

    mGluR Neurological Disease
    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  • HY-128770
    LY3154207

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
  • HY-15141
    Staurosporine

    Antibiotic AM-2282; STS; AM-2282

    PKC PKA Apoptosis Bacterial Fungal Antibiotic Cancer Infection
    Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine is an apoptosis inducer.
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-16716
    Basmisanil

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  • HY-12683
    BPTES

    Glutaminase Cancer
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  • HY-59047
    Tolimidone

    MLR-1023

    Src Metabolic Disease
    Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
  • HY-101858
    BQCA

    mAChR Neurological Disease
    BQCA a highly selective allosteric modulator of the M1 mAChR.
  • HY-101845
    FITM

    mGluR Cancer
    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  • HY-13831
    BPTU

    BMS-646786

    P2Y Receptor Cancer Neurological Disease
    BPTU is a novel P2Y1 allosteric antagonist.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-10721
    PF-AKT400

    AKT protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-18296
    AKT-IN-1

    Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-112788
    ONO-8590580

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • HY-P0222
    PKI(5-24)

    PKA Others
    PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-15857
    CW-069

    Kinesin Cancer
    CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-B0764A
    Bucladesine calcium

    Dibutyryl cAMP calcium salt; DBcAMP calcium salt

    PKA Phosphodiesterase (PDE) Apoptosis Others
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
  • 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-P0222A
    PKI(5-24) TFA

    PKA Others
    PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-13260
    CCT128930

    Akt Autophagy Cancer
    CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
  • HY-116009
    RMC-4550

    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-112094
    WNK-IN-11

    Others Others
    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  • HY-13449
    TAK-733

    MEK Cancer
    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
  • HY-15476
    VU 0364439

    mGluR Neurological Disease
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
  • 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-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-100519
    NVS-PAK1-1

    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-19559
    JNJ-46778212

    VU 0409551

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

    mAChR Others
    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
  • HY-13340
    VU0152100

    VU152100

    mAChR Neurological Disease
    VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
  • HY-15252
    Reparixin L-lysine salt

    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-101068
    TOFA

    RMI14514; MDL14514

    Acetyl-CoA Carboxylase Cancer
    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  • HY-70037
    Cinacalcet

    AMG 073

    CaSR Cardiovascular Disease
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • 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-18601
    (±)-BI-D

    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

    SSR

    FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-15713
    NMS-873

    p97 Cancer
    NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with 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-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-11012
    TDZD-8

    GSK-3β Inhibitor I; NP 01139

    GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
  • HY-14417B
    VU0155041 sodium

    mGluR Neurological Disease
    VU0155041 sodium is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 sodium is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAMP sodium salt; DBcAMP sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • 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-70037A
    Cinacalcet hydrochloride

    AMG-073 hydrochloride

    CaSR Cardiovascular Disease
    Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-109046
    Tulrampator

    CX-1632

    iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • 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-15393
    VU 0357121

    mGluR Neurological Disease
    VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.
  • HY-12408
    6H05

    Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-136172
    ESI-08

    Ras Cancer Metabolic Disease Cardiovascular Disease
    ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
  • HY-15618
    MK-7622

    M1 receptor modulator

    mAChR Neurological Disease
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
  • 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-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-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    AChE Apoptosis Neurological Disease
    Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.
  • HY-12408A
    6H05 (TFA)

    Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • 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-111446
    EPAC 5376753

    Others 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-14419
    TCN238

    mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • 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-P2285
    AC 253

    Amyloid-β
    AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
  • HY-114169
    WRG-28

    Discoidin Domain Receptor Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
  • HY-13058
    ADX-47273

    mGluR Neurological Disease
    ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
  • 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

    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-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-125880
    SBI-553

    Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-18654
    ADX88178

    mGluR Neurological Disease
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  • HY-12682
    Glutaminase C-IN-1

    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-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-16071
    AT13148

    Akt PKA ROCK Ribosomal S6 Kinase (RSK) Cancer
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
  • HY-N2180
    Pinoresinol dimethyl ether

    (+)-Eudesmin

    Others Neurological Disease
    Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furofuran lignan isolated from the stem bark of Magnolia kobus with neuritogenic activity. Pinoresinol dimethyl ether ((+)-Eudesmin) can induce neuritis outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.
  • 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-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-50081
    CCR2-RA-[R]

    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-12042
    Pimasertib

    AS703026; MSC1936369B

    MEK Cancer
    Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
  • HY-17601
    Alofanib

    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-12152
    PNU-120596

    NSC 216666

    nAChR Neurological Disease
    PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM.
  • HY-14609A
    MPEP

    mGluR Neurological Disease
    MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
  • 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-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-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-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC Cancer
    Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-12059A
    AT7867 dihydrochloride

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-100530
    Rp-cAMPS triethylammonium salt

    PKA Neurological Disease
    Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-12059
    AT7867

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-111759
    Jaspamycin

    7-CN-7-C-Ino

    PKA Parasite Infection
    Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity.
  • 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-15748
    JNJ-40411813

    ADX-71149

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

    mGluR Neurological Disease
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
  • HY-119217
    AZ084

    CCR Inflammation/Immunology Endocrinology
    AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma.
  • HY-124622
    NNC-0640

    Glucagon Receptor 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-19715
    SGC707

    Histone Methyltransferase Cancer
    SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.
  • 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-16951
    VU-1545

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

    mGluR Neurological Disease
    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  • HY-10595
    Ro 28-1675

    Glucokinase Metabolic Disease
    Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-111184
    PIK-108

    PI3K Cancer
    PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
  • 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-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-108262
    UCN-02

    7-epi-Hydroxystaurosporine

    PKC PKA Cancer
    UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively. UCN-02 (7-epi-Hydroxystaurosporine) displays cytotoxic effect on the growth of HeLa S3 cells.
  • 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-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-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-114164
    Thrombin

    Thrombin Neurological Disease
    Thrombin is a trypsin-like allosteric serine protease. Thrombin enables site-specific cleavage of fusion proteins with an accessible Thrombin recognition sequence and can be used to digest GST-tagged proteins.
  • 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.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • 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-108708
    GeA-69

    PARP Cancer
    GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
  • 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-13619
    Efaproxiral

    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-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-114368
    Kira8

    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-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-19752A
    VU0357017 hydrochloride

    CID-25010775

    mAChR Neurological Disease
    VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
  • 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-114304
    COH000

    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-13619A
    Efaproxiral sodium

    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-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-18652
    Ro 5126766

    CH5126766

    MEK Raf Cancer
    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-100932
    ML-9

    Myosin Cancer
    ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • HY-108254
    Bisindolylmaleimide IV

    Arcyriarubin A

    PKC CMV Infection
    Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
  • HY-15424
    5-Iodotubercidin

    NSC 113939; 5-ITu

    Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.
  • HY-10933
    Ampalex

    CX516; BDP 12; Ampakine CX516

    iGluR Neurological Disease
    Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
  • HY-104010
    Asciminib

    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-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-10341
    Fasudil Hydrochloride

    HA-1077 Hydrochloride; AT-877 Hydrochloride

    ROCK Calcium Channel Autophagy PKA PKC HIV Cancer
    Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
  • HY-10230S
    Midostaurin-D5

    PKC412-D5; CGP 41251-D5

    Others Cancer
    Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 (hydrochloride)

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-P1125
    4-CMTB

    Others Others
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
  • HY-101455
    CDN1163

    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-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-111763
    GPR40/FFAR1 modulator 1

    GPR40 Metabolic Disease
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  • HY-10299
    GSK-923295

    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-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-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-112942A
    CMP-Sialic acid sodium salt

    CMP-Neu5Ac sodium salt

    Others Metabolic Disease
    CMP-Sialic acid sodium salt (CMP-Neu5Ac sodium salt) is an allosteric inhibitor of UDP-GlcNAc 2-epimerase, the enzyme that initiates sialic acid synthesis. CMP-Sialic acid sodium salt provides a substrate for Golgi sialyltransferases.
  • HY-19719
    Miransertib

    ARQ-092

    Akt Cancer
    Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
  • 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-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.
  • 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-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-108467
    GGsTop

    Nahlsgen

    Others Cardiovascular Disease
    GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
  • HY-10341A
    Fasudil

    HA-1077; AT877

    ROCK Calcium Channel Autophagy PKA PKC Cancer
    Fasudil (HA-1077; AT877), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator.
  • HY-16743
    Ibiglustat

    Venglustat; SAR402671; GZ402671

    Others Metabolic Disease
    Ibiglustat (Venglustat), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • 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-114314
    BA-53038B

    HBV Infection
    BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
  • HY-112209
    VU0467154

    mAChR Neurological Disease
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    GABA Receptor Neurological Disease
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • HY-103269
    BAI1

    Bcl-2 Family Cancer
    BAI1 is a selective and allosteric inhibitor of BAX activation. BAI1 demonstrates inhibition of tBID (HY-100464)-induced BAX-mediated membrane permeabilization with an IC50 of 3.3 μΜ.
  • HY-13848
    AZD8797

    CXCR Inflammation/Immunology Endocrinology
    AZD8797 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-100932A
    ML-9 Free Base

    Myosin Cancer
    ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • HY-N6732
    K-252a

    SF2370; Antibiotic K 252a; Antibiotic SF 2370

    PKC PKA CaMK Trk Receptor Autophagy Infection
    K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-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-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-103040
    Zuranolone

    GABA Receptor Neurological Disease
    Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-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-103575A
    MFZ 10-7 hydrochloride

    mGluR Neurological Disease
    MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
  • HY-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-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-15445
    CTEP

    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.
  • 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-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-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-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-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-117571
    BPN14770

    Phosphodiesterase (PDE) Neurological Disease
    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-115502
    BCI

    (E)-BCI

    Phosphatase Cancer Inflammation/Immunology
    BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
  • 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-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-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-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-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-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-12429
    Beclabuvir

    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-N2118
    Bilobetin

    PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-115502A
    BCI hydrochloride

    (E)-BCI hydrochloride

    Phosphatase Cancer Inflammation/Immunology
    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
  • HY-16743A
    Ibiglustat L-Malic acid

    Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)

    Others Metabolic Disease
    Ibiglustat L-Malic acid (Venglustat L-Malic acid), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • 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-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic 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-10355
    AKT inhibitor VIII

    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-112603
    AP5

    GPR40 Metabolic Disease
    AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
  • HY-10519
    BMS-345541

    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-10518
    BMS-345541 hydrochloride

    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-P1259A
    PR-39 TFA

    Proteasome Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 stimulates angiogenesis and inhibits inflammatory responses by specifically blocking degradation of IkappaBalpha and HIF-1alpha by the proteasome.
  • HY-P1259
    PR-39

    Proteasome Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 stimulates angiogenesis and inhibits inflammatory responses by specifically blocking degradation of IkappaBalpha and HIF-1alpha by the proteasome.
  • HY-116819
    VU0453379

    Glucagon Receptor 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-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-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-10358
    MK-2206 dihydrochloride

    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-10198
    Navarixin

    SCH 527123; MK-7123

    CXCR Inflammation/Immunology Endocrinology
    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-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) for the treatment of cognition/memory 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-N6791
    KT5823

    PKA PKC Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • HY-12316
    20(S)-Hydroxycholesterol

    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-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-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-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU 0361737 (ML-128) is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
  • 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-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-N0281
    Daphnetin

    7,8-Dihydroxycoumarin

    EGFR PKA PKC Autophagy Parasite Inflammation/Immunology Cancer
    Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative isolated from plants of the Genus Daphne, is a 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 (7,8-dihydroxycoumarin) is a secondary metabolite of plants used in folk medicine to counter inflammatory and allergic diseases, also has has the potential in the treatment of coagulation disorders, rheumatoid arthritis with anti-malarian and anti-pyretic properties.
  • 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-12150
    CCMI

    nAChR Neurological Disease
    CCMI 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-13965
    Parmodulin 2

    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-P1397
    RVD-Hpα

    Cannabinoid Receptor
    RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-127111
    NDI-091143

    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-10046
    Plerixafor

    AMD 3100; JM3100; SID791

    CXCR HIV Virus Protease 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-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-112769
    EX229

    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-123872
    MSC1094308

    p97 Others
    MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
  • 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-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    mTOR FKBP Autophagy Cancer
    Rapamycin-d3 (Sirolimus-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. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-101478
    Fenobam

    mGluR Neurological Disease
    Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 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-50688
    SB-265610

    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-110279
    Ogerin

    Others Neurological Disease
    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
  • HY-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-N0240
    Herbacetin

    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-117282
    JG-98

    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

    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-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 drug 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-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-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-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-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-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-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • 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, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
  • 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-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. Anticancer activities.
  • 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-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-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-16708A
    ZLN024 hydrochloride

    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-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-119374
    BRM/BRG1 ATP Inhibitor-1

    Others Cancer
    BRM/BRG1 ATP Inhibitor-1 is an 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[1] .
  • HY-117287
    BMS-986165

    JAK Interleukin Related IFNAR Inflammation/Immunology
    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. BMS-986165 inhibits IL-12/23 and type I IFN pathways.
  • 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-P1045
    187-1, N-WASP inhibitor

    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-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-13509
    CCG-50014

    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-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-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
  • 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-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-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

    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-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-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-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-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-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase 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.
  • 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-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-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 has the potential for epilepsy.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy 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-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.