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158

Inhibitors & Agonists

2

Screening Libraries

1

Dye Reagents

15

Peptides

13

Natural
Products

11

Recombinant Proteins

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-103187
    HEMADO

    Adenosine Receptor Cancer Inflammation/Immunology
    HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype.
  • HY-103229
    Cl-HIBO

    iGluR Neurological Disease
    Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties.
  • HY-P2287
    Cortagine

    CRFR Neurological Disease
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
  • HY-109085
    Difamilast

    OPA-15406

    Phosphodiesterase (PDE) Inflammation/Immunology
    Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).
  • HY-B1833
    Afloqualone

    HQ-495

    GABA Receptor Neurological Disease
    Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous and sedative effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
  • 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-100369A
    DMCM hydrochloride

    GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5  receptors, respectively.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-103066
    Br-PBTC

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.
  • HY-128855
    Talsaclidine

    mAChR Neurological Disease
    Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
  • HY-126005
    VGSC blocker-1

    Sodium Channel Cancer
    VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability.
  • HY-133012
    GFB-8438

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
  • HY-109014
    Tenofovir exalidex

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.
  • HY-101844
    ML-18

    Bombesin Receptor Cancer
    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  • HY-B2192
    Amylase

    Others Metabolic Disease
    Amylase is an enzyme produced by pancreas and salivary glands, catalyzing the hydrolysis of starch into sugars. Amylase are broadly classified into α, β, and γ subtypes.
  • HY-115766
    Anabaseine

    nAChR Neurological Disease
    Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes.
  • HY-114380
    Radioprotectin-1

    LPL Receptor Others
    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
  • HY-15393
    VU 0357121

    mGluR Neurological Disease
    VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
  • HY-N2309
    Kainic acid

    Others Neurological Disease
    Kainic acid is a potent agonist at excitatory amino acid receptor subtypes in the CNS.
  • HY-17015A
    Peramivir

    RWJ-270201; BCX-1812

    Influenza Virus Infection
    Peramivir (RWJ-270201;BCX-1812) is a highly potent, selective and orally active influenza virus neuraminidase (NA) inhibitor, with IC50 values ranging form 0.9 to 4.3 nM for nine NA subtypes.
  • HY-B0374A
    Moxonidine hydrochloride

    BDF5895 hydrochloride

    Imidazoline Receptor Neurological Disease
    Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
  • HY-17015
    Peramivir trihydrate

    RWJ 270201 trihydrate; BCX 1812 trihydrate

    Influenza Virus Infection
    Peramivir trihydrate (RWJ-270201 trihydrate;BCX-1812 trihydrate) is a highly potent, selective and orally active influenza virus neuraminidase (NA) inhibitor, with IC50 values ranging from 0.9 to 4.3 nM for nine NA subtypes.
  • 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-115764
    nAChR agonist 2

    nAChR Neurological Disease
    nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).
  • HY-103120
    Org37684

    5-HT Receptor Neurological Disease
    Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor.
  • HY-U00030
    Rispenzepine

    mAChR Neurological Disease
    Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.
  • HY-B0374
    Moxonidine

    BDF5895

    Imidazoline Receptor Neurological Disease
    Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
  • HY-P1423A
    BA 1 TFA

    Bombesin Receptor Cancer Metabolic Disease
    BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
  • HY-P1423
    BA 1

    Bombesin Receptor Cancer Metabolic Disease
    BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
  • HY-109013
    Sofpironium bromide

    BBI 4000

    mAChR Neurological Disease
    Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.
  • HY-10914
    UCPH-101

    Others Neurological Disease
    UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
  • HY-B0197A
    Naratriptan hydrochloride

    GR-85548A hydrochloride

    5-HT Receptor Neurological Disease
    Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.
  • HY-B0197
    Naratriptan

    GR-85548A

    5-HT Receptor Neurological Disease
    Naratriptan is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.
  • HY-B0197AS
    Naratriptan D3 Hydrochloride

    GR-85548A D3

    5-HT Receptor Neurological Disease
    Naratriptan D3 Hydrochloride is the deuterium labeled Naratriptan, which is a selective 5-HT1 receptor subtype agonist.
  • 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-12439
    ML380

    mAChR Neurological Disease
    ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
  • HY-19505
    TPA-023B

    GABA Receptor Neurological Disease
    TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
  • HY-P0036
    Octreotide

    SMS 201-995

    Somatostatin Receptor Inflammation/Immunology Cardiovascular Disease Endocrinology
    Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
  • 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-10797
    CJ-42794

    CJ-042794

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
  • HY-B1339
    Dicyclomine hydrochloride

    Dicycloverine hydrochloride

    mAChR Neurological Disease
    Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo.
  • HY-119078
    VU0080241

    mGluR Neurological Disease
    VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM.
  • HY-101640
    TPA 023

    GABA Receptor Neurological Disease
    TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
  • HY-12405
    CGP-42112

    CGP42112A

    Angiotensin Receptor Neurological Disease Endocrinology
    CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
  • HY-101869
    MK-0343

    MRK-409

    GABA Receptor Neurological Disease
    MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
  • HY-P1132
    Galanin (1-29)(rat, mouse)

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively. Anticonvulsant effect.
  • HY-P1132A
    Galanin (1-29)(rat, mouse) TFA

    Neuropeptide Y Receptor Neurological Disease
    Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect.
  • HY-101308
    MRS2179 tetrasodium

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
  • HY-129150
    Ganoderic acid TR

    Influenza Virus Infection
    Ganoderic acid TR is a broad-spectrum inhibitor against influenza neuraminidases (NAs), particularly H5N1 and H1N1 neuraminidases. The IC50 values of 10.9 and 4.6 μM, respectively.
  • HY-101308A
    MRS2179 tetrasodium hydrate

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.
  • HY-114962
    S-22153

    Melatonin Receptor Neurological Disease
    S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes.
  • HY-B0979
    Lobeline hydrochloride

    α-Lobeline hydrochloride; L-Lobeline hydrochloride

    nAChR Neurological Disease
    Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
  • HY-111271A
    L 888607 Racemate

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
  • HY-124498
    Oxantel

    CP-14445

    nAChR Parasite Infection
    Oxantel (CP-14445), a m-oxyphenol derivative of Pyrantel (HY-12641), is a N-subtype AChR agonist. Oxantel is an anthelmintic, with excellent trichuricidal properties.
  • HY-Y0313
    p-Hydroxybenzaldehyde

    Endogenous Metabolite GABA Receptor Neurological Disease
    p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
  • HY-D1398
    LtIA-F

    Others Neurological Disease
    LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
  • HY-118504
    Sulfoxaflor

    nAChR Neurological Disease
    Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens.
  • HY-14608
    L-Glutamic acid

    Endogenous Metabolite iGluR Ferroptosis Apoptosis Neurological Disease
    L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-15072
    Zonampanel

    YM 872

    iGluR Metabolic Disease
    Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
  • HY-N0584A
    Anisodamine hydrobromide

    6-Hydroxyhyoscyamine hydrobromide

    mAChR Inflammation/Immunology
    Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties.
  • HY-14608A
    L-Glutamic acid monosodium salt

    iGluR Apoptosis Ferroptosis Neurological Disease
    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  • HY-122878
    HS-131

    HSP Cancer
    HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers.
  • HY-12811
    PF-04856264

    Sodium Channel Neurological Disease
    PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
  • HY-116594
    OPC-14523 free base

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
  • HY-B0371B
    (R)-Terazosin

    Adrenergic Receptor Endocrinology
    (R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
  • HY-107725
    BIBO3304 TFA

    Neuropeptide Y Receptor Metabolic Disease
    BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively).
  • 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-B1154
    Penbutolol sulfate

    (-)-Terbuclomine

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Penbutolol sulfate is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker.
  • HY-14565
    Pozanicline

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
  • 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-100858
    PP7

    Influenza Virus Infection
    PP7 is a potent PB1-PB2 interaction inhibitor with an IC50 of 8.6 μM, and their inhibition against viral polymerase activity (IC50=9.5 μM). PP7 shows antiviral activities against influenza A virus (IAV), including A(H1N1)pdm09 (EC50=1.4 μM), A(H7N9) and A(H9N2) subtypes.
  • HY-B0374S
    Moxonidine-d4

    Imidazoline Receptor Neurological Disease
    Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine. Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
  • HY-102037
    SSTR5 antagonist 1

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a)
  • HY-103183
    CV1808

    2-Phenylaminoadenosine

    Adenosine Receptor Endogenous Metabolite Inflammation/Immunology
    CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively.
  • 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-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-114191
    SSTR5 antagonist 2

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  • 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-114191A
    SSTR5 antagonist 2 TFA

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  • HY-13225A
    Rivanicline

    RJR-2403; (E)-Metanicotine

    nAChR Neurological Disease
    Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).
  • HY-N0584
    Anisodamine

    6-Hydroxyhyoscyamine

    mAChR Neurological Disease
    Anisodamine (6-Hydroxyhyoscyamine), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning.
  • HY-P1202A
    CYN 154806 TFA

    Somatostatin Receptor Endocrinology
    CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
  • HY-116594A
    OPC-14523 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
  • HY-101254
    Luzindole

    N-0774

    Melatonin Receptor Neurological Disease
    Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.
  • 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-P1202
    CYN 154806

    Somatostatin Receptor Endocrinology
    CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
  • HY-P1268
    α-Conotoxin PIA

    nAChR Neurological Disease
    α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-102094
    (E/Z)-SIB-1893

    mGluR Neurological Disease
    (E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist.
  • HY-136459
    NMDA receptor antagonist 2

    iGluR Neurological Disease
    NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
  • HY-P1268A
    α-Conotoxin PIA TFA

    nAChR Neurological Disease
    α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-14277A
    Levocabastine hydrochloride

    R 50547 hydrochloride

    Histamine Receptor Neurotensin Receptor Inflammation/Immunology
    Levocabastine (R 50547) hydrochloride is a long acting, highly potent and selective histamine H1-receptor antagonist with anti-allergic activity. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2.
  • HY-13225
    Rivanicline oxalate

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    nAChR Neurological Disease
    Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-14567
    Ciproxifan

    FUB-359

    Histamine Receptor Neurological Disease Endocrinology
    Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease.
  • 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-13225B
    Rivanicline hemioxalate

    RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate

    nAChR Neurological Disease
    Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-15289
    Ciproxifan maleate

    FUB 359 maleate

    Histamine Receptor Neurological Disease Endocrinology
    Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
  • HY-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
  • HY-D0976
    NF279

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env.
  • HY-42110
    Deschloroclozapine

    mAChR Neurological Disease
    Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [ 11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.
  • HY-101630
    Deramciclane

    EGIS-3886

    5-HT Receptor Neurological Disease
    Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
  • HY-108592
    UCL 2077

    Others Neurological Disease
    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.
  • HY-14813
    Cutamesine

    SA4503; AGY 94806

    Sigma Receptor Neurological Disease
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  • HY-119226
    VU0152099

    mAChR Neurological Disease
    VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
  • HY-108669
    AZ10606120 dihydrochloride

    P2X Receptor Cancer Neurological Disease
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-15688
    8-Hydroxy-DPAT hydrobromide

    8-OH-DPAT hydrobromide

    5-HT Receptor Neurological Disease
    8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
  • HY-111539
    BAY-1316957

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent drug metabolism and pharmacokinetics properties, and can be used for endometriosis research.
  • HY-122267
    Clovamide

    trans-Clovamide

    Reactive Oxygen Species Bacterial Influenza Virus Apoptosis Inflammation/Immunology Neurological Disease
    Clovamide (trans-Clovamide), a natural phenolic compound, is a potent antioxidant. Clovamide is an excellent ROS and oxygen radical scavenger. Clovamide also has anti-inflammatory and neuroprotective effects. Clovamide is an anti-microbial with activity against the human pathogens influenza A subtype H5N1, Trypanosoma evansi, and Heliobacter pylori.
  • HY-B1562
    Bopindolol

    (±)-Bopindolol

    Adrenergic Receptor Cardiovascular Disease
    Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be used for essential and renovascular hypertension research.
  • HY-79135
    Pasireotide ditrifluoroacetate

    SOM230 ditrifluoroacetate; Pasireotide TFA salt

    Somatostatin Receptor Endocrinology Cancer
    Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-P1221
    ProTx II

    Sodium Channel Neurological Disease
    ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.
  • HY-12993
    RSV604

    A-60444

    RSV Infection
    RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM).
  • HY-131179
    Influenza A virus-IN-1

    Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
  • HY-11048
    NS11394

    GABA Receptor Neurological Disease
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
  • HY-108768
    Pasireotide pamoate

    SOM230 pamoate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-111964
    Lenacapavir

    GS-6207

    HIV Infection
    Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs).
  • HY-111501
    H4R antagonist 1

    Histamine Receptor Inflammation/Immunology Endocrinology
    H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
  • HY-110092
    PSB-1114 tetrasodium

    P2Y Receptor Metabolic Disease
    PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors.
  • HY-B0391A
    Naftopidil dihydrochloride

    KT-611 dihydrochloride; BM-15275 dihydrochloride

    Adrenergic Receptor Cancer
    Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
  • HY-131973
    PDE10A-IN-2 hydrochloride

    Phosphodiesterase (PDE) Metabolic Disease Cardiovascular Disease
    PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
  • HY-110135A
    NBI-31772 hydrate

    IGF-1R Neurological Disease
    NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.
  • HY-122560A
    VU0134992 hydrochloride

    Potassium Channel Cardiovascular Disease
    VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • HY-B0391B
    Naftopidil hydrochloride

    KT-611 hydrochloride; BM-15275 hydrochloride

    Adrenergic Receptor Cancer
    Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
  • HY-B0391
    Naftopidil

    KT-611; BM-15275

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
  • HY-79136
    Pasireotide L-aspartate salt

    SOM230 L-aspartate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-106100
    Roxindole

    EMD 49980

    Dopamine Receptor Serotonin Transporter Neurological Disease
    Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities.
  • HY-107628
    DH97

    Melatonin Receptor Neurological Disease
    DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses.
  • HY-122560
    VU0134992

    Potassium Channel Cardiovascular Disease
    VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • HY-103212
    Azepexole dihydrochloride

    B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM).
  • HY-111557
    YM-254890

    P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
  • HY-107508
    VU-29

    mGluR Neurological Disease
    VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
  • HY-128686
    KAG-308

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.
  • HY-14350
    AC-55541

    Protease-Activated Receptor (PAR) Others
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo.
  • 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-18596
    SB-215505

    5-HT Receptor Neurological Disease
    SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
  • HY-135483A
    AR-R17779 hydrochloride

    nAChR Neurological Disease
    AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways.
  • 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-10121
    Asenapine

    Org 5222

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor Neurological Disease Endocrinology
    Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
  • HY-16381A
    Pasireotide acetate

    SOM230 acetate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-32329
    Setiptiline

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-P1220
    Huwentoxin-IV

    Sodium Channel Neurological Disease
    Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-13285
    Ki16425

    Debio 0719

    LPL Receptor Neurological Disease Cancer
    Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
  • HY-16381
    Pasireotide

    SOM230

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-136207
    TC-2559 difumarate

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
  • HY-P1220A
    Huwentoxin-IV TFA

    Sodium Channel Neurological Disease
    Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-32329A
    Setiptiline maleate

    MO-8282

    5-HT Receptor Neurological Disease
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-17606
    Cenerimod

    ACT-334441

    LPL Receptor Inflammation/Immunology
    Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
  • HY-106353
    Smilagenin

    Endogenous Metabolite mAChR Neurological Disease
    Smilagenin (SMI) is a small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density. Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD.
  • HY-141547
    Nav1.7-IN-8

    Sodium Channel Cytochrome P450 Inflammation/Immunology
    Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-126291
    GNE-616

    Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.
  • 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-32329S
    Setiptiline-d3

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-138879B
    CP-601932

    (1S,5R)-CP-601927

    nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS.
  • HY-W009009
    L-838417

    GABA Receptor Neurological Disease
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
  • HY-125777A
    α-Conotoxin Vc1.1 TFA

    nAChR Neurological Disease
    α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.
  • HY-108495
    CYM50308

    ML248

    LPL Receptor Cardiovascular Disease
    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
  • HY-12583
    A-366

    Histone Methyltransferase Epigenetic Reader Domain Cancer
    A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
  • HY-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.