Search Result
Results for "Aldehyde Dehydrogenase (ALDH) Agonists" in MCE Product Catalog:
1479
Inhibitors & Agonists
2
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-135841
-
|
CM10
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
Metabolic Disease
|
|
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity.
|
-
- HY-76006
-
-
- HY-19801
-
|
CVT-10216
|
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
|
|
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
|
-
- HY-W016645
-
-
- HY-122577
-
-
- HY-18768
-
|
NCT-501
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-W012570
-
-
- HY-18768A
-
|
NCT-501 hydrochloride
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-136594
-
|
BODIPY aminoacetaldehyde
BAAA
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
|
-
- HY-131633A
-
-
- HY-124011
-
-
- HY-W020014
-
-
- HY-140620
-
-
- HY-133456
-
-
- HY-136051
-
-
- HY-136077
-
-
- HY-136074
-
-
- HY-B0240
-
|
Disulfiram
Tetraethylthiuram disulfide; TETD
|
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
|
Metabolic Disease
Cancer
|
|
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
|
-
- HY-113165A
-
-
- HY-136054
-
-
- HY-135977
-
-
- HY-117041
-
-
- HY-133457
-
-
- HY-W004305
-
-
- HY-138064
-
|
4-APC hydrobromide
|
Others
|
Others
|
|
4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.
|
-
- HY-136076
-
-
- HY-18936
-
-
- HY-136091
-
-
- HY-N1177
-
-
- HY-136140
-
-
- HY-133465
-
-
- HY-33914
-
-
- HY-12465
-
-
- HY-N2597
-
-
- HY-Z0031
-
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N0018
-
|
Daidzin
Daidzoside; NPI-031D; Daidzein 7-O-glucoside
|
Mitochondrial Metabolism
Reverse Transcriptase
|
Others
|
|
Daidzin is an isoflavone that has anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.
|
-
- HY-W012926
-
-
- HY-135658
-
-
- HY-126241
-
|
RV01
|
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
|
|
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
|
-
- HY-13259
-
|
MG-132
Z-Leu-Leu-Leu-al; MG132
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
|
-
- HY-114702
-
|
M77976
|
PDHK
|
Metabolic Disease
|
|
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
|
-
- HY-103665
-
|
STING agonist-3
|
STING
|
Cancer
|
|
STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
|
-
- HY-B0876
-
|
Fomepizole
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.
|
-
- HY-15394
-
-
- HY-P1333A
-
|
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-P1334A
-
-
- HY-113013
-
|
Hydroxypyruvic acid
β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-113013A
-
|
Hydroxypyruvic acid lithium hydrate
β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-N2548
-
-
- HY-113466
-
|
4-Hydroxynonenal
4-HNE
|
Aldehyde Dehydrogenase (ALDH)
Endogenous Metabolite
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
-
- HY-17462
-
|
Adrenosterone
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
|
|
Adrenosterone ((+)-Adrenosterone) is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone also is a selective and competitive inhibitor of hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1).
|
-
- HY-124697
-
|
BMP signaling agonist sb4
|
TGF-β Receptor
|
Cancer
|
|
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
|
-
- HY-79494
-
-
- HY-12745A
-
|
Nalfurafine hydrochloride
TRK-820 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
|
-
- HY-12745
-
|
Nalfurafine
TRK-820
|
Opioid Receptor
|
Neurological Disease
|
|
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
|
-
- HY-113165
-
-
- HY-10019
-
|
Varenicline
CP 526555
|
nAChR
|
Neurological Disease
|
|
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
|
-
- HY-W007330
-
-
- HY-W008393
-
-
- HY-W004307
-
-
- HY-113076
-
-
- HY-N0084
-
|
Betulinaldehyde
Betulinic Aldehyde; Betunal
|
Bacterial
|
Infection
Cancer
|
|
Betulinaldehyde(Betunal) belongs to pentacyclic triterpenoids and was reported to exhibit antimicrobial activities against bacteria and fungi, including S.
|
-
- HY-I0637
-
-
- HY-W011417
-
|
Cinnabarinic acid
|
mGluR
Apoptosis
|
Others
|
|
Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
|
-
- HY-14302
-
-
- HY-17453
-
-
- HY-135119
-
|
Salmeterol-D3
|
Adrenergic Receptor
|
Endocrinology
Inflammation/Immunology
|
|
Salmeterol-D3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
|
-
- HY-18761
-
|
Cobalt phthalocyanine
Cobalt(II) phthalocyanine; Cobaltous phthalocyanine; Phthalocyanine cobalt complex
|
Others
|
Others
|
|
Cobalt phthalocyanine is a catalyst of redox reaction, catalyzes aerobic regenerations of aldehydes and ketones from aldoximes and ketoximes has been developed.
|
-
- HY-N7624
-
|
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
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- HY-15453
-
|
Devimistat
CPI-613
|
Apoptosis
|
Cancer
|
|
Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
|
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-133112
-
-
- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
Apoptosis
|
Cancer
Neurological Disease
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
|
-
- HY-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-101603
-
-
- HY-P1201
-
|
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-Y0790
-
|
Cuminaldehyde
|
Endogenous Metabolite
|
Cancer
|
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.
|
-
- HY-129545
-
-
- 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-Y0015
-
|
p-Dimethylaminobenzaldehyde
4-DimethylaminobenzAldehyde
|
Others
|
Others
|
|
p-Dimethylaminobenzaldehyde (4-Dimethylaminobenzaldehyde) is an organic compound containing amine and aldehyde moieties which is used in Ehrlich's reagent and Kovac's reagent to test for indoles.
|
-
- HY-P1201A
-
|
Cyclosomatostatin TFA
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-W012530
-
-
- HY-13673
-
|
Goserelin
ICI 118630
|
GNRH Receptor
Apoptosis
|
Endocrinology
|
|
Goserelin, a gonadotropin-releasing hormone (GnRH) analogue, functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-N0295
-
|
Protocatechualdehyde
CatechAldehyde; Protocatechuic Aldehyde; Rancinamycin IV
|
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
|
|
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent.
|
-
- HY-W008129
-
-
- HY-N2498
-
-
- HY-13673A
-
|
Goserelin acetate
ICI-118630 acetate
|
GNRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Goserelin acetate (ICI-118630 acetate), a gonadotropin-releasing hormone (GnRH) analogue, functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-103476
-
|
Ro15-4513
|
GABA Receptor
|
Neurological Disease
|
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
|
-
- HY-101966
-
|
NCT-503
|
Others
|
Cancer
|
|
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
|
-
- HY-112645
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-100020
-
-
- HY-17038A
-
|
Agomelatine hydrochloride
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038
-
|
Agomelatine
S-20098
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-B1021
-
|
Vincamine
|
GPR40
|
Metabolic Disease
Cardiovascular Disease
|
|
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.
|
-
- HY-W011094
-
|
Win 18446
|
Aldehyde Dehydrogenase (ALDH)
|
Endocrinology
|
|
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
|
-
- HY-17038B
-
|
Agomelatine (L(+)-Tartaric acid)
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-100991
-
|
FG 7142
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
|
-
- HY-14281
-
|
Trilostane
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
|
-
- HY-100742B
-
-
- HY-13986
-
|
Merimepodib
VX-497; MMPD
|
HBV
HCV
|
Infection
|
|
Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
|
-
- HY-77521
-
-
- HY-W014787
-
-
- HY-124062
-
|
TAS-114
|
Others
|
Cancer
|
|
TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
|
-
- HY-100681
-
-
- HY-103096
-
|
R162
|
Others
|
Cancer
|
|
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
|
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-111095
-
|
D-(-)-Lactic acid
(R)-2-Hydroxypropionic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants.
|
-
- HY-135675
-
-
- HY-133023
-
|
Indium(III) isopropoxide
|
Others
|
Others
|
|
Indium(III) Isopropoxide is an organo-metallic compound. Indium(III) Isopropoxide uesd as a hydrogen transfer catalyst for conversion of benzylic alcohols into aldehydes or ketones via Oppenauer oxidation. Indium(III) Isopropoxide also can be used as metal precursor.
|
-
- HY-B0199
-
|
Mycophenolate Mofetil
RS 61443; TM-MMF
|
Apoptosis
|
Cancer
|
|
Mycophenolate Mofetil is an immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-N6736
-
|
K-252c
|
PKC
Bacterial
Apoptosis
|
Cancer
Infection
|
|
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
|
-
- HY-111108
-
|
LDH-IN-1
|
Lactate Dehydrogenase
|
Cancer
|
|
LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
|
-
- HY-113304
-
-
- HY-W001941
-
|
D-Cystine
|
Others
|
Others
|
|
D-Cystine is the D-enantiomer of L-Cystine. D-Cystine inhibits L-aspartate-β-semialdehyde dehydrogenase (ASADH) from Escherichia coli.
|
-
- HY-113128
-
-
- HY-W001187
-
|
Tempo
|
DNA/RNA Synthesis
Reactive Oxygen Species
Mitochondrial Metabolism
|
Cancer
|
|
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects.
|
-
- HY-N7961
-
-
- HY-18055
-
-
- HY-113128A
-
-
- HY-18053
-
-
- HY-113166
-
-
- HY-113128B
-
-
- HY-16214
-
|
FX-11
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
|
Cancer
|
|
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell，a Ki value of 8 μM.
|
-
- HY-17469
-
|
Gimeracil
Gimestat
|
Others
|
Cancer
|
|
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).
|
-
- HY-108325
-
-
- HY-B2004
-
|
Thifluzamide
|
Fungal
|
Infection
|
|
Thifluzamide, a broad-spectrum succinate dehydrogenase inhibitor (SDHI) fungicide, has been widely used in the controlling of a variety of fungal diseases in rice fields.
|
-
- HY-N7114A
-
-
- HY-135570
-
-
- HY-12688
-
|
Succinyl phosphonate
|
Endogenous Metabolite
Reactive Oxygen Species
|
Neurological Disease
|
|
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-W040073
-
|
Nifurtimox
|
Parasite
Lactate Dehydrogenase
|
Cancer
Infection
|
|
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
|
-
- HY-N2337
-
-
- HY-129630
-
-
- HY-12688A
-
|
Succinyl phosphonate trisodium salt
|
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Metabolic Disease
Neurological Disease
|
|
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-18717
-
-
- HY-100742
-
-
- HY-128578
-
-
- HY-135654
-
-
- HY-W017522
-
|
Adipic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.
|
-
- HY-135648
-
-
- HY-W012875
-
-
- HY-113212
-
|
Ursocholic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
|
-
- HY-136498
-
|
T-705RMP
|
Drug Metabolite
|
Infection
|
|
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
|
-
- HY-N3115
-
|
Palbinone
|
Others
|
Inflammation/Immunology
|
|
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
|
-
- HY-101943
-
|
LY 345899
|
Others
|
Cancer
|
|
LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1.
|
-
- HY-117240
-
|
NCT-502
|
Others
|
Cancer
|
|
NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.
|
-
- HY-16082
-
|
AZD7545
|
PDHK
|
Metabolic Disease
|
|
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
|
-
- HY-113108
-
|
(R)-3-Hydroxyisobutyric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
|
-
- HY-128787
-
-
- HY-100742A
-
|
(R)-GNE-140
|
Lactate Dehydrogenase
|
Cancer
|
|
(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
|
-
- HY-123962
-
-
- HY-101930
-
|
BMS-816336
|
Others
|
Metabolic Disease
|
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
|
-
- HY-19540
-
-
- HY-W051723
-
|
(R)-3-Hydroxybutanoic acid
(R)-(-)-3-Hydroxybutanoic acid; (R)-3-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(R)-3-Hydroxybutanoic acid is a metabolite, and converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid has applications as a nutrition source and as a precursor for vitamins, antibiotics and pheromones.
|
-
- HY-W078844
-
|
PfDHODH-IN-2
|
Dihydroorotate Dehydrogenase
Parasite
|
Infection
|
|
PfDHODH-IN-2, a dihydrothiophenone derivative (Compound 11), is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC50 of 1.11 µM. PfDHODH-IN-2 acts as an antimalarial agent and can be used for the research of malaria.
|
-
- HY-10533
-
|
Eniluracil
5-Ethynyluracil; GW776C85
|
Others
|
Cancer
|
|
Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
|
-
- HY-12492
-
|
VER-246608
|
PDHK
|
Cancer
|
|
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
|
-
- HY-100184
-
-
- HY-114009
-
-
- HY-101232
-
|
Tiotidine
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
|
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-B1729
-
|
Phenoxyethanol
|
Bacterial
|
Infection
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.
|
-
- HY-100688
-
|
ML390
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models.
|
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-N2177
-
|
3-Dehydrotrametenolic acid
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
|
-
- HY-N7393
-
|
Isomalt
Palatinitol
|
Lactate Dehydrogenase
|
Metabolic Disease
|
|
Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes.
|
-
- HY-W040307
-
|
Saccharopine
L-Saccharopine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis.
|
-
- HY-W015851
-
|
(R)-3-Hydroxybutanoic acid sodium
(R)-(-)-3-Hydroxybutanoic acid sodium; (R)-3-Hydroxybutyric acid sodium
|
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-Hydroxybutanoic acid sodium ((R)-3-Hydroxybutyric acid) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium has applications as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones.
|
-
- HY-114459
-
-
- HY-126254
-
|
BI-4924
|
Others
|
Cancer
|
|
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
|
-
- HY-103394
-
|
TC HSD 21
|
Others
|
Cancer
|
|
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
|
-
- HY-14234
-
-
- HY-12762
-
|
QS11
|
Others
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-123943
-
|
STING agonist-4
|
STING
|
Cancer
|
|
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function.
|
-
- HY-131145
-
-
- HY-112921B
-
-
- HY-112921A
-
-
- HY-100699
-
-
- HY-118539
-
-
- HY-131974
-
-
- HY-13423
-
-
- HY-130251
-
|
DS18561882
|
Others
|
Cancer
|
|
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.
|
-
- HY-N0157
-
|
Orotic acid
6-Carboxyuracil; Vitamin B13
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-N0157A
-
|
Orotic acid zinc
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-B2245
-
-
- HY-107399
-
-
- HY-17354A
-
-
- HY-17354
-
-
- HY-P0236A
-
-
- HY-110304
-
-
- HY-136435
-
-
- HY-114400
-
-
- HY-113377
-
|
L-Glyceric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Glyceric acid is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid excretion to distinguish PH1 from PH2.
|
-
- HY-113377A
-
|
L-Glyceric acid sodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Glyceric acid sodium is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid sodium can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid sodium excretion to distinguish PH1 from PH2.
|
-
- HY-10545
-
|
Taribavirin
|
HBV
HCV
|
Infection
|
|
Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-18767
-
|
Ivosidenib
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Metabolic Disease
|
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-10545A
-
|
Taribavirin hydrochloride
|
HBV
HCV
|
Infection
|
|
Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-101930B
-
|
(R)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
|
-
- 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-19574
-
-
- HY-135400
-
-
- HY-13239
-
-
- HY-112597
-
-
- HY-131105S
-
-
- HY-P1738
-
-
- HY-109131
-
-
- HY-N0108
-
|
Physcion
Parietin; Rheochrysidin
|
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
|
-
- HY-102053
-
-
- HY-135399
-
-
- HY-111353
-
-
- HY-107688A
-
|
UB-165 fumarate
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
|
-
- HY-131104S
-
-
- HY-103039
-
-
- HY-136449
-
-
- HY-100699S
-
-
- HY-P1144
-
-
- HY-131104AS
-
-
- HY-100087
-
-
- HY-135954A
-
|
PDK4-IN-1 hydrochloride
|
PDHK
Apoptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
|
-
- HY-101813
-
|
Laflunimus
HR325
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.
|
-
- HY-W010342
-
|
6-Aminonicotinamide
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
|
-
- HY-18056
-
|
PF-915275
|
Others
|
Metabolic Disease
|
|
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
|
-
- HY-10020
-
|
Varenicline Hydrochloride
CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
|
-
- HY-103083
-
-
- HY-P1144A
-
-
- HY-101039A
-
-
- HY-112679
-
-
- HY-13288
-
-
- HY-108415
-
-
- HY-U00340
-
|
PPAR agonist 1
|
PPAR
|
Metabolic Disease
|
|
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
|
-
- HY-100012
-
|
CBR-5884
|
Others
|
Cancer
|
|
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
|
-
- HY-18173
-
|
AZD8329
|
Others
|
Metabolic Disease
|
|
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
|
-
- HY-111583
-
|
RXFP3/4 agonist 1
|
Others
|
Metabolic Disease
|
|
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.
|
-
- HY-19711
-
|
STING agonist-1
G10
|
STING
Virus Protease
|
Infection
|
|
STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
|
-
- HY-17405
-
-
- HY-100810
-
-
- HY-12405
-
-
- HY-112185
-
-
- HY-136608
-
-
- HY-136609
-
-
- HY-B1161
-
|
Methoprene
ZR-515
|
Others
|
Infection
|
|
Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist.
|
-
- HY-12835
-
-
- HY-13653
-
-
- HY-15510B
-
|
Tenovin-6 Hydrochloride
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-114226
-
|
Olutasidenib
FT-2102
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Inflammation/Immunology
|
|
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
|
-
- HY-114855
-
|
BT2
|
Bcl-2 Family
|
Metabolic Disease
|
|
BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
|
-
- HY-15510
-
|
Tenovin-6
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-42068
-
-
- HY-B1829A
-
-
- HY-101717
-
-
- HY-U00281
-
-
- HY-U00227
-
-
- HY-100234A
-
-
- HY-100234
-
-
- HY-W002116
-
-
- HY-107743
-
|
Naloxone benzoylhydrazone
NalBzoH
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.
|
-
- HY-101265
-
|
S1p receptor agonist 1
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.
|
-
- HY-130243
-
|
RORγt Inverse agonist 6
|
ROR
|
Inflammation/Immunology
|
|
RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
|
-
- HY-114310
-
|
VDR agonist 1
|
VD/VDR
Apoptosis
|
Cancer
|
|
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.
|
-
- HY-108566
-
-
- HY-B1540
-
-
- HY-P1000
-
-
- HY-19065
-
-
- HY-P0187
-
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-100380
-
-
- HY-P1313A
-
-
- HY-18776
-
-
- HY-P2518
-
-
- HY-114411
-
-
- HY-10559
-
|
Nelotanserin
APD125
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
- HY-P1504
-
-
- HY-B0716S
-
-
- HY-10013
-
|
Taranabant
MK-0364
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
|
-
- HY-U00205
-
-
- HY-50108
-
-
- HY-U00123
-
-
- HY-U00066
-
-
- HY-A0173
-
-
- HY-17416A
-
-
- HY-A0129
-
-
- HY-N1415
-
-
- HY-107901
-
|
Pparδ agonist 1
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
|
-
- HY-P1504A
-
-
- HY-14304
-
-
- HY-B0418A
-
-
- HY-131338
-
-
- HY-14340
-
|
WAY-181187
SAX-187
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
|
-
- 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-N0808
-
-
- HY-A0008
-
-
- HY-B0316
-
|
Avobenzone
|
Estrogen Receptor/ERR
Apoptosis
|
Others
|
|
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
|
-
- HY-P0108
-
-
- HY-B2215
-
-
- HY-B0489
-
-
- HY-14917
-
-
- HY-19998
-
-
- HY-16722
-
-
- HY-17633
-
-
- HY-U00230
-
-
- HY-N2309
-
-
- HY-107480
-
-
- HY-14799
-
-
- HY-14864A
-
-
- HY-P0236
-
-
- HY-B0380A
-
-
- HY-B0380
-
-
- HY-14864
-
-
- HY-108449
-
-
- HY-101585
-
-
- HY-P1013
-
-
- HY-100113
-
-
- HY-14773S
-
-
- HY-128922
-
-
- HY-108472
-
-
- HY-16713A
-
-
- HY-U00216
-
-
- HY-13201
-
-
- HY-100532
-
-
- HY-103173
-
-
- HY-16713
-
-
- HY-B0189
-
-
- HY-33353
-
-
- HY-111132
-
-
- HY-B0570
-
-
- HY-U00226
-
-
- HY-13201A
-
-
- HY-U00293
-
-
- HY-B0475
-
-
- HY-U00038
-
-
- HY-12451
-
-
- HY-P1481
-
-
- HY-N2411
-
-
- HY-19320
-
-
- HY-109527
-
-
- HY-41076
-
-
- HY-13736A
-
-
- HY-P1337
-
-
- HY-14299
-
-
- HY-19661
-
-
- HY-113035
-
-
- HY-P1470
-
-
- HY-P1336
-
-
- HY-14299A
-
-
- HY-17355A
-
-
- HY-101274
-
-
- HY-B0188
-
-
- HY-B0189A
-
-
- HY-P1532
-
-
- HY-W015326
-
-
- HY-111068
-
-
- HY-17622
-
-
- HY-21098A
-
-
- HY-12664
-
-
- HY-P1480
-
-
- HY-101973
-
-
- HY-B0374A
-
-
- HY-U00233
-
-
- HY-135572
-
-
- HY-14958A
-
-
- HY-14958
-
-
- HY-P1123
-
|
MEDICA16
|
ATP Citrate Lyase
GPR40
GPR120
|
Metabolic Disease
|
|
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120.
|
-
- HY-19434A
-
|
cis-ACPD
|
iGluR
mGluR
|
Neurological Disease
|
|
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
|
-
- HY-P1198
-
-
- HY-17366A
-
|
Clozapine N-oxide dihydrochloride
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-17366
-
|
Clozapine N-oxide
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-114146
-
-
- HY-100124
-
-
- HY-P1087
-
-
- HY-B0452
-
-
- HY-101038A
-
-
- HY-B0091A
-
-
- HY-11077
-
-
- HY-113035A
-
-
- HY-B0091
-
-
- HY-P1578
-
-
- HY-10448
-
-
- HY-79593
-
-
- HY-B0409A
-
-
- HY-101582
-
-
- HY-19250
-
-
- HY-103704
-
-
- HY-107216
-
-
- HY-N2371
-
-
- HY-B0648
-
-
- HY-12499
-
-
- HY-19468
-
-
- HY-P1337A
-
-
- HY-P0252
-
-
- HY-P1192
-
-
- HY-14773
-
-
- HY-W014666
-
-
- HY-109197
-
-
- HY-101639A
-
-
- HY-102075A
-
-
- HY-100336
-
-
- HY-10475
-
|
AM580
CD336; NSC608001; Ro 40-6055
|
RAR/RXR
Autophagy
|
Cancer
|
|
AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
|
-
- HY-15108
-
-
- HY-101384A
-
-
- HY-P1331
-
-
- HY-100140
-
-
- HY-41700
-
-
- HY-107319
-
-
- HY-12749
-
-
- HY-B1403
-
-
- HY-101299
-
-
- HY-16972
-
|
SR9243
|
LXR
|
Cancer
|
|
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
|
-
- HY-N6629
-
-
- HY-104026
-
-
- HY-100291
-
-
- HY-P1578A
-
-
- HY-101987
-
-
- HY-13101
-
-
- HY-P0226
-
-
- HY-19883
-
-
- HY-N0178
-
-
- HY-A0040
-
-
- HY-P1515
-
-
- HY-101639
-
-
- HY-13788B
-
-
- HY-10002
-
-
- HY-P1198A
-
-
- HY-14304A
-
|
Zinterol hydrochloride
MJ 9184 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits.
|
-
- HY-P0078
-
|
TRAP-6
PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6
|
Protease-Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
|
-
- HY-N0166
-
-
- HY-114464
-
|
11-Beta-hydroxyandrostenedione
4-Androsten-11β-ol-3,17-dione
|
Endogenous Metabolite
|
Endocrinology
|
|
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
|
-
- HY-100775
-
|
Setogepram sodium salt
PBI-4050 sodium salt
|
GPR40
GPR84
|
Metabolic Disease
Inflammation/Immunology
|
|
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram sodium salt decreases renal, liver and pancreatic fibrosis. Setogepram sodium salt exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
|
-
- HY-B0436
-
-
- HY-14229
-
-
- HY-B0188A
-
-
- HY-100140A
-
-
- HY-14785
-
-
- HY-W014325
-
-
- HY-101864
-
-
- HY-19334
-
-
- HY-14785A
-
-
- HY-P0079
-
-
- HY-114116
-
-
- HY-10838
-
-
- HY-P0297
-
-
- HY-15306
-
-
- HY-P1477
-
-
- HY-12749A
-
-
- HY-N3216
-
-
- HY-16465
-
-
- HY-12721
-
-
- HY-18939
-
-
- HY-14648A
-
-
- HY-107418
-
-
- HY-P1515A
-
-
- HY-P2321
-
-
- HY-101271
-
-
- HY-P0088
-
-
- HY-100166
-
-
- HY-10480
-
-
- HY-111454
-
-
- HY-15677
-
-
- HY-13421
-
-
- HY-16086
-
-
- HY-101492
-
-
- HY-P0226A
-
-
- HY-15388
-
-
- HY-B0374
-
-
- HY-B0769
-
-
- HY-10922
-
-
- HY-136258
-
|
nAChR agonist CMPI hydrochloride
|
nAChR
|
Neurological Disease
|
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
|
-
- HY-115400
-
|
1V209
TLR7 agonist T7
|
Toll-like Receptor (TLR)
|
Cancer
|
|
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
|
-
- 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-P1145
-
-
- HY-70037
-
-
- HY-107542
-
-
- HY-112627
-
-
- HY-111786
-
-
- HY-102016
-
-
- HY-101540
-
-
- HY-B0716
-
-
- HY-14870
-
-
- HY-108003
-
-
- HY-76772A
-
-
- HY-15885
-
-
- HY-B0206
-
-
- HY-14734
-
-
- HY-107395
-
-
- HY-15291
-
-
- HY-19919
-
|
BMS-779788
EXEL04286652; XL-652; BMS-788
|
LXR
|
Metabolic Disease
|
|
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
|
-
- HY-14171
-
|
Bexarotene
LGD1069
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-100347A
-
-
- HY-15566
-
|
APD597
JNJ-38431055
|
GPR119
|
Metabolic Disease
|
|
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
|
-
- HY-108414
-
-
- HY-18723
-
-
- HY-14734A
-
-
- HY-101822
-
-
- HY-19308
-
-
- HY-16737
-
-
- HY-19434
-
|
trans-ACPD
Trans-(±)-ACP
|
mGluR
|
Metabolic Disease
|
|
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
|
-
- HY-P1334
-
-
- HY-17551
-
-
- HY-131103
-
-
- HY-P2321A
-
-
- HY-103107
-
-
- HY-76772B
-
-
- HY-P1477A
-
-
- HY-16998
-
|
SR2211
|
ROR
|
Inflammation/Immunology
|
|
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
|
-
- HY-30006
-
-
- HY-10233
-
|
Gaboxadol hydrochloride
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays
a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic and has hypnotic activities.
|
-
- HY-15430A
-
-
- HY-106094
-
-
- HY-B0084
-
-
- HY-136586
-
-
- HY-P1533
-
-
- HY-B1583
-
-
- HY-17457
-
-
- HY-P1031
-
-
- HY-B0735
-
-
- HY-112322
-
-
- HY-100728
-
-
- HY-19945
-
|
DAA-1106
|
GABA Receptor
|
Neurological Disease
|
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
- HY-12111
-
-
- HY-B0566
-
-
- HY-100673
-
-
- HY-P1145A
-
-
- HY-101331
-
-
- HY-114025
-
-
- HY-70037A
-
-
- HY-17355B
-
-
- HY-U00206
-
-
- HY-111271
-
-
- HY-12584
-
-
- HY-B0735A
-
-
- HY-B0726
-
-
- HY-50935
-
-
- HY-B1832
-
-
- HY-P1339
-
-
- HY-101273
-
-
- HY-P1545
-
-
- HY-111498
-
-
- HY-B1752A
-
-
- HY-P1577
-
-
- HY-W015878
-
-
- HY-B0468
-
-
- HY-100942
-
-
- HY-19511
-
|
GSK2018682
|
LPL Receptor
|
Inflammation/Immunology
|
|
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
|
-
- HY-14546
-
-
- HY-14261
-
-
- HY-103225
-
-
- HY-114165
-
-
- HY-P0059
-
|
Teriparatide
Human parathyroid hormone-(1-34); hPTH (1-34)
|
Others
|
Cancer
|
|
Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC50 of 2 nM in HEK293 cells.
|
-
- HY-18100A
-
-
- HY-B1006
-
-
- HY-101950
-
-
- HY-B0194A
-
-
- HY-101420
-
-
- HY-103187
-
-
- HY-17030
-
-
- HY-12199
-
-
- HY-B0197A
-
-
- HY-P1339A
-
-
- HY-12520A
-
-
- HY-16162A
-
-
- HY-B0577
-
-
- HY-109096
-
-
- HY-12199B
-
-
- HY-A0014
-
-
- HY-B0194
-
-
- HY-101386
-
-
- HY-15601
-
-
- HY-P1467
-
-
- HY-15778
-
-
- HY-P1545A
-
-
- HY-P0098
-
-
- HY-P2273
-
-
- HY-B0197
-
-
- HY-112152
-
-
- HY-101609
-
-
- HY-14149
-
-
- HY-P1349
-
-
- HY-16465A
-
-
- HY-B0197AS
-
-
- HY-B0354A
-
-
- HY-50911
-
-
- HY-15306A
-
-
- HY-13788C
-
-
- HY-136429
-
|
Ethylhydrocupreine
Optochin
|
Bacterial
Parasite
|
Infection
|
|
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-136429A
-
|
Ethylhydrocupreine hydrochloride
Optochin hydrochloride
|
Bacterial
Parasite
|
Infection
|
|
Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-N0175
-
|
Cytisinicline
Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
|
|
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
|
-
- HY-P1467A
-
-
- HY-107675
-
-
- HY-16728
-
|
Rapastinel
GLYX-13
|
iGluR
|
Neurological Disease
|
|
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
|
-
- HY-P1164
-
-
- HY-17034B
-
-
- HY-B0459
-
-
- HY-101586
-
-
- HY-12199A
-
-
- HY-16916
-
-
- HY-101649
-
-
- HY-P1588
-
-
- HY-13510
-
-
- HY-N0382
-
|
Galangin
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-13715
-
-
- HY-13788
-
-
- HY-13788A
-
-
- HY-103410
-
-
- HY-P0244
-
-
- HY-100856
-
-
- HY-B0383A
-
-
- HY-14953
-
|
Imepitoin
AWD 131-138
|
GABA Receptor
|
Neurological Disease
|
|
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
|
-
- HY-14652
-
-
- HY-101419
-
-
- HY-12237
-
-
- HY-14426
-
-
- HY-P2279
-
-
- HY-101787
-
-
- HY-14831
-
|
Arhalofenate
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
- HY-19317
-
-
- HY-15243
-
-
- HY-13715A
-
-
- HY-N2311
-
|
Ibotenic acid
(RS)-Ibotenic acid; DL-Ibotenic acid
|
iGluR
|
Neurological Disease
|
|
Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites.
|
-
- HY-B0802
-
-
- 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-14413
-
|
SR3335
ML 176
|
ROR
|
Metabolic Disease
|
|
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
|
-
- HY-19775
-
-
- HY-101300
-
-
- HY-P1309A
-
-
- HY-A0007
-
-
- HY-131961
-
|
Triciferol
|
VD/VDR
HDAC
|
Cancer
|
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
|
-
- HY-A0182A
-
-
- HY-B0545
-
-
- HY-N0783
-
-
- HY-19365
-
-
- HY-P1164A
-
-
- HY-P0244A
-
-
- HY-17501
-
|
Bambuterol
(±)-Bambuterol; KWD-2183
|
Adrenergic Receptor
|
Endocrinology
|
|
Bambuterol ((±)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
|
-
- HY-B0447A
-
-
- HY-P1127
-
-
- HY-10629
-
-
- HY-17584
-
|
Linaclotide
|
Guanylate Cyclase
|
Others
|
|
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-P1012
-
-
- HY-128604
-
|
XY101
|
ROR
|
Cancer
|
|
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
|
-
- HY-111200
-
-
- HY-108526
-
-
- HY-17501A
-
|
Bambuterol hydrochloride
(±)-Bambuterol hydrochloride; KWD-2183 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
Bambuterol hydrochloride ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
|
-
- HY-109104
-
-
- HY-15536A
-
-
- HY-P0210
-
-
- HY-10487
-
-
- HY-13338S
-
-
- HY-12216
-
-
- HY-U00371
-
-
- HY-A0182
-
-
- HY-P0090
-
|
Calcitonin (salmon)
Salmon calcitonin
|
CGRP Receptor
|
Cancer
|
|
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
|
-
- HY-B0659
-
-
- HY-19863
-
-
- HY-101192
-
-
- HY-B0383
-
-
- HY-P0014
-
-
- HY-16504
-
-
- HY-18687
-
-
- HY-126047B
-
|
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-111406
-
|
Omidenepag isopropyl
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug.
|
-
- HY-111098
-
-
- HY-15848
-
-
- HY-13773
-
-
- HY-P0298
-
-
- HY-13443
-
-
- HY-B1893
-
-
- HY-102075B
-
|
TMP780
|
ROR
|
Inflammation/Immunology
|
|
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
|
-
- HY-P1012A
-
-
- HY-14601
-
-
- HY-15443
-
-
- HY-19134
-
-
- HY-B0606
-
-
- HY-14557
-
-
- HY-B0418AS
-
-
- HY-19946
-
-
- HY-P0210B
-
-
- HY-109044
-
-
- HY-P0298A
-
-
- HY-B1473
-
-
- HY-14342
-
-
- HY-P1533A
-
-
- HY-16728B
-
|
Rapastinel Trifluoroacetate
GLYX-13 Trifluoroacetate
|
iGluR
|
Neurological Disease
|
|
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
|
-
- HY-101442
-
|
SR9238
|
LXR
|
Metabolic Disease
|
|
SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
|
-
- HY-14792
-
|
Inolitazone
Efatutazone; CS-7017; RS5444
|
PPAR
|
Cancer
|
|
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
|
-
- HY-B0823
-
|
Acetamiprid
|
nAChR
|
Neurological Disease
|
|
Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.
|
-
- HY-14887
-
-
- HY-10021
-
-
- HY-101640
-
-
- HY-13443A
-
-
- HY-U00215
-
|
Ro 41-3290
|
GABA Receptor
|
Neurological Disease
|
|
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor. Ro 41-3290 is an investigational hypnotic.
|
-
- HY-13467
-
-
- HY-B0121
-
-
- HY-75502
-
-
- HY-N0322
-
|
Cholesterol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Metabolic Disease
|
|
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
|
-
- HY-121744
-
|
PS10
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
|
-
- HY-B0031S
-
-
- HY-14792B
-
|
Inolitazone dihydrochloride
Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride
|
PPAR
|
Cancer
|
|
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
|
-
- HY-114269
-
-
- HY-A0007S
-
-
- HY-16988A
-
-
- HY-A0190
-
-
- HY-N6709
-
|
Zeranol
α-Zearalanol
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
|
-
- HY-13044
-
-
- HY-17568
-
|
Nonivamide
Pelargonic acid vanillylamide; Nonanoic acid vanillylamide; Pseudocapsaicin
|
TRP Channel
|
Neurological Disease
|
|
Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
|
-
- HY-B1347
-
-
- HY-B0106A
-
-
- HY-111110
-
-
- HY-124540B
-
-
- HY-19995
-
-
- HY-100013C
-
-
- HY-N0169
-
-
- HY-13715B
-
-
- HY-100032
-
-
- HY-101929
-
-
- HY-50844
-
|
Ibutamoren Mesylate
MK-677; MK-0677
|
GHSR
|
Endocrinology
|
|
Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.
|
-
- HY-16989
-
|
SR9009
|
Autophagy
|
Cancer
|
|
SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-13967B
-
-
- HY-B0659A
-
-
- HY-Y0966
-
-
- HY-14557A
-
-
- HY-16988
-
|
SR9011
|
Autophagy
|
Cancer
|
|
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-14817
-
-
- HY-135601
-
-
- HY-101869
-
-
- HY-B0447
-
-
- HY-P1481A
-
-
- HY-14167
-
-
- HY-P1322
-
-
- HY-P1314
-
-
- HY-P1869
-
-
- HY-N0377
-
-
- HY-P1170
-
-
- HY-P0119A
-
-
- HY-100881
-
-
- HY-100441
-
-
- HY-B0459A
-
-
- HY-B0163
-
-
- HY-P1308
-
-
- HY-B0100
-
|
Etomidate
R 16659
|
GABA Receptor
|
Neurological Disease
|
|
Etomidate (R 16659) is a potent GABAA receptor agonist. Etomidate is a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.
|
-
- HY-101238
-
-
- HY-P2519
-
-
- 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-N0361
-
|
Dihydrocapsaicin
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.
|
-
- HY-50919
-
|
Paricalcitol
|
VD/VDR
|
Metabolic Disease
|
|
Paricalcitol, a vitamin D analogue, is a vitamin D receptor agonist, used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.
|
-
- HY-14839
-
-
- HY-B1478
-
-
- HY-101907
-
-
- HY-N7707
-
|
Sandacanol
|
Apoptosis
|
Cancer
|
|
Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
|
-
- HY-125824
-
-
- HY-119433
-
|
Asoprisnil
J867
|
Progesterone Receptor
|
Endocrinology
|
|
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
|
-
- HY-B0556
-
|
Tetrahydrozoline
Tetryzoline
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tetrahydrozoline (Tetryzoline), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline is widely used for the research of nasal congestion and conjunctival congestion.
|
-
- HY-P0165
-
-
- HY-16642A
-
-
- HY-130115A
-
|
IACS-8803 disodium
|
STING
|
Cancer
|
|
IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy.
|
-
- HY-B0556A
-
-
- HY-U00373
-
-
- HY-12761
-
-
- HY-16684
-
|
AGN 195183
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.
|
-
- HY-P1030
-
-
- HY-14824
-
|
Sofiniclin
ABT 894
|
nAChR
|
Neurological Disease
|
|
Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD).
|
-
- HY-15382
-
-
- HY-B0163A
-
-
- HY-B1111
-
-
- HY-B1037
-
-
- HY-100490B
-
|
Rilmenidine phosphate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-100490
-
|
Rilmenidine
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
|
-
- HY-110160
-
|
Pozanicline dihydrochloride
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
|
-
- HY-P1322A
-
-
- HY-N0049
-
|
Nuciferine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- 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-10013B
-
-
- HY-13556A
-
|
Arzoxifene hydrochloride
LY 353381 HCl; SERM 3
|
Estrogen Receptor/ERR
|
Cancer
|
|
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
|
-
- HY-128113
-
-
- HY-12705A
-
-
- HY-12381
-
|
ML224
NCGC00242364; ANTAG3
|
TSH Receptor
|
Endocrinology
|
|
ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
|
-
- HY-B0100A
-
|
Etomidate hydrochloride
R16659 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Etomidate hydrochloride (R 16659 hydrochloride) is a potent GABAA receptor agonist. Etomidate hydrochlorideis a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.
|
-
- HY-P2541
-
-
- HY-14417A
-
-
- HY-B0524A
-
-
- HY-U00183
-
-
- HY-131103S
-
-
- HY-B1052
-
-
- HY-N2253
-
-
- HY-105634A
-
|
Nomegestrol acetate
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
|
-
- HY-B1052A
-
-
- HY-103698A
-
-
- HY-P1314A
-
-
- HY-111492
-
|
DIM-C-pPhOCH3
|
Others
|
Cancer
|
|
DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
|
-
- HY-103207
-
-
- HY-D0237
-
-
- HY-12434
-
-
- HY-111498A
-
-
- HY-B0524
-
-
- HY-P0288
-
-
- HY-14218
-
-
- HY-15027
-
-
- HY-125946
-
-
- HY-100490A
-
|
Rilmenidine hemifumarate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-10626
-
|
T0901317
|
LXR
FXR
ROR
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
|
-
- HY-13291
-
-
- HY-101454
-
-
- HY-B0031S1
-
-
- HY-P1160
-
-
- HY-P0185
-
-
- HY-103252
-
-
- HY-100443A
-
-
- HY-10013A
-
-
- HY-10627A
-
-
- HY-130012
-
-
- HY-14414
-
|
GSK4112
SR6452
|
Autophagy
|
Metabolic Disease
|
|
GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.
|
-
- HY-19770
-
|
GSK2981278
|
ROR
|
Inflammation/Immunology
|
|
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
|
-
- HY-P0186
-
-
- HY-U00435
-
-
- HY-15606
-
|
Tanaproget
NSP-989
|
Progesterone Receptor
|
Endocrinology
|
|
Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.
|
-
- HY-N0132A
-
-
- HY-U00450
-
-
- HY-N0132
-
-
- HY-19381
-
-
- HY-111343
-
|
ONC212
|
Apoptosis
|
Cancer
Endocrinology
|
|
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
|
-
- HY-A0279A
-
|
Pristinamycin IA
Mikamycin B; Mikamycin IA
|
Bacterial
|
Others
|
|
Pristinamycin IA (Mikamycin B;Mikamycin IA), a biologically active decapeptide isolated from the skin of the Australian frog Hyla caerulea, is a potent cholecystokinetic agent, and acts as a cholecystokinin receptor agonist.
|
-
- 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-13008
-
-
- HY-P1308A
-
-
- HY-N3977
-
|
Grifolic acid
|
GPR120
|
Inflammation/Immunology
|
|
Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
|
-
- HY-P0199
-
-
- HY-121251
-
-
- HY-104042
-
|
Vorasidenib
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
|
-
- HY-P1333
-
|
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-19650
-
-
- HY-114118
-
-
- HY-110238
-
|
MK6-83
|
TRP Channel
|
Metabolic Disease
|
|
MK6-83 is a new candidate agonist of TRPML1 with an improved efficacy and potency. MK6-83 has the potential for Mucolipidosis type IV study.
|
-
- HY-A0181A
-
-
- HY-17043
-
-
- HY-20019
-
|
L-165041
|
PPAR
|
Metabolic Disease
|
|
L-165041 is a cell permeable PPARδ agonist, with Kis of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.
|
-
- HY-13740
-
-
- HY-101325
-
-
- HY-N2148
-
|
Cytosporone B
Csn-B; Dothiorelone G
|
Others
|
Cancer
|
|
Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
|
-
- HY-112219A
-
-
- 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-105634
-
|
Nomegestrol
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-101372A
-
|
Oxotremorine M iodide
|
mAChR
|
Neurological Disease
|
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
|
-
- HY-100815B
-
|
(RS)-AMPA
(±)-AMPA
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors.
|
-
- HY-P1180
-
-
- HY-120384
-
|
AZD-0284
|
ROR
|
Inflammation/Immunology
|
|
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.
|
-
- HY-13861
-
-
- HY-B1415
-
|
Clofibric acid
Chlorofibrinic acid
|
PPAR
Drug Metabolite
|
Others
|
|
Clofibric acid (Chlorofibrinic acid), the pharmaceutically active metabolite of lipid regulators Clofibrate, Etofibrate and Etofyllinclofibrate, is a PPARα agonist which exhibits hypolipidemic effects. Clofibric acid also is an herbicide.
|
-
- HY-A0010
-
-
- HY-123291
-
-
- HY-106147
-
|
Frakefamide
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-18295
-
-
- HY-112606
-
|
ML-290
|
Others
|
Others
|
|
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM.
|
-
- HY-15484
-
-
- HY-16639
-
-
- HY-N6691
-
|
Veratridine
3-Veratroylveracevine
|
Sodium Channel
|
Neurological Disease
|
|
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
|
-
- HY-19996
-
|
AH-7614
|
GPR120
|
Metabolic Disease
|
|
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
|
-
- HY-10349A
-
|
WAY-100635 Maleate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.
|
-
- HY-119222
-
|
GSK256073
|
GPR109A
|
Metabolic Disease
|
|
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-131032
-
|
KI-7
|
Adenosine Receptor
|
Others
|
|
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively.
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-15124
-
-
- HY-B0584
-
|
Travoprost
Fluprostenol isopropyl ester; AL6221; Flu-Ipr
|
Prostaglandin Receptor
|
Endocrinology
|
|
Travoprost (Fluprostenol isopropyl ester), an isopropyl ester prodrug, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension.
|
-
- HY-111809
-
-
- HY-15564
-
|
AR 231453
|
GPR119
|
Metabolic Disease
|
|
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
|
-
- HY-B0820
-
|
Nitenpyram
|
nAChR
|
Neurological Disease
|
|
Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.
|
-
- HY-P1180A
-
-
- HY-106157
-
-
- HY-105170B
-
|
ABT-418 hydrochloride
|
nAChR
|
Neurological Disease
|
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
|
-
- HY-13720A
-
|
Pergolide mesylate
Pergolide methanesulfonate; LY127809
|
Dopamine Receptor
|
Neurological Disease
|
|
Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research.
|
-
- HY-G0014B
-
-
- HY-106025
-
|
Radequinil
AC-3933
|
GABA Receptor
|
Neurological Disease
|
|
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
|
-
- 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-G0014A
-
-
- HY-18760
-
|
LY2812223
|
mGluR
|
Neurological Disease
|
|
LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
|
-
- HY-100155
-
|
4-IBP
|
Sigma Receptor
|
Cancer
|
|
4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
|
-
- HY-18678A
-
-
- HY-101085
-
|
SKL2001
|
Wnt
β-catenin
|
Cancer
|
|
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
|
-
- HY-106007
-
-
- HY-B1270
-
-
- HY-135392
-
-
- HY-14608
-
-
- HY-P1160A
-
-
- HY-15043
-
-
- HY-131106S
-
-
- HY-12694
-
-
- HY-B0287
-
|
Clofibrate
|
PPAR
|
Metabolic Disease
|
|
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
|
-
- HY-15655
-
-
- HY-13410
-
|
Xanomeline oxalate
LY246708 oxalate
|
mAChR
|
Neurological Disease
|
|
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.
|
-
- HY-10678
-
|
BMS-687453
|
PPAR
|
Cardiovascular Disease
|
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-106147B
-
|
Frakefamide TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
|
-
- HY-19937
-
|
Saroglitazar
|
PPAR
|
Metabolic Disease
|
|
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-W013372
-
-
- HY-N0163
-
-
- HY-16751
-
-
- HY-105124A
-
-
- HY-105040C
-
|
Pomaglumetad methionil hydrochloride
LY2140023 hydrochloride
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.
|
-
- HY-104049
-
|
Lanifibranor
IVA337
|
PPAR
|
Metabolic Disease
Cancer
|
|
Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
|
-
- HY-P1016A
-
-
- HY-14221
-
|
Siramesine
Lu 28-179
|
Sigma Receptor
Ferroptosis
|
Cancer
|
|
Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
|
-
- HY-N6642
-
|
Ankaflavin
|
PPAR
|
Cancer
Inflammation/Immunology
|
|
Ankaflavin, isolated from Monascus-Fermented red rice, is a PPARγ agonist with anti-inlfammatory activity. Ankaflavin exhibits selective cytotoxic effect and induces cell death on cancer cells.
|
-
- HY-P2625
-
-
- HY-17416
-
-
- HY-19937A
-
|
Saroglitazar Magnesium
|
PPAR
|
Metabolic Disease
|
|
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-12222
-
|
Obeticholic acid
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
|
-
- HY-10622
-
-
- HY-100806
-
-
- HY-17034
-
-
- HY-14221A
-
|
Siramesine hydrochloride
Lu 28-179 hydrochloride
|
Sigma Receptor
Ferroptosis
|
Cancer
|
|
Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
|
-
- HY-112217A
-
|
PSEM 89S TFA
|
nAChR
|
Neurological Disease
|
|
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
|
-
- HY-107982
-
|
VU6005649
|
mGluR
|
Neurological Disease
|
|
VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
|
-
- HY-11035
-
|
WAY-262611
|
β-catenin
|
Cancer
|
|
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.
|
-
- HY-114118A
-
-
- HY-107512
-
-
- HY-12560D
-
-
- HY-13713
-
-
- HY-13715C
-
-
- HY-136290
-
-
- HY-10680
-
|
MK-6892
|
GPR109A
|
Cancer
|
|
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
|
-
- HY-B2054
-
|
Tebufenozide
|
Apoptosis
|
Others
|
|
Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.
|
-
- HY-113970A
-
|
Nebracetam hydrochloride
WEB 1881 FU hydrochloride
|
mAChR
|
Neurological Disease
|
|
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i.
|
-
- HY-14608A
-
-
- HY-N6825
-
-
- HY-103546
-
-
- HY-116214
-
|
Cyprodinil
|
Fungal
Androgen Receptor
|
Infection
Endocrinology
|
|
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
- HY-103409
-
|
ABT-724 trihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
|
-
- HY-16056
-
|
Arbutamine
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist that increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine is a catecholamine for a pharmacological cardiac stress agen.
|
-
- HY-19870
-
-
- HY-104070
-
|
LG-100064
|
RAR/RXR
Autophagy
|
Cancer
|
|
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
|
-
- HY-P1317
-
-
- HY-17642
-
|
Omidenepag
|
Prostaglandin Receptor
|
Endocrinology
|
|
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2.
|
-
- HY-133113
-
-
- HY-128770
-
-
- HY-P0186A
-
-
- HY-120160
-
|
Darglitazone
CP-86325
|
PPAR
|
Metabolic Disease
Neurological Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-10957
-
|
L-692429
MK-0751
|
GHSR
|
Metabolic Disease
|
|
L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.
|
-
- HY-18941
-
|
Eglumegad
LY354740; Eglumetad
|
mGluR
|
Neurological Disease
|
|
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
|
-
- HY-103007
-
-
- HY-P1731B
-
|
Tirzepatide hydrochloride
LY3298176 hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
|
Tirzepatide hydrochloride (LY3298176 hydrochloride) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.
|
-
- HY-19870B
-
-
- HY-14554
-
-
- HY-108529
-
|
BMS493
|
RAR/RXR
|
Metabolic Disease
|
|
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation.
|
-
- HY-128064
-
-
- HY-13956
-
|
Pioglitazone
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
|
-
- HY-110241
-
|
Dianicline dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
|
-
- HY-B1500
-
-
- HY-N0164
-
|
Matrine
Matridin-15-one; Vegard; α-Matrine
|
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
|
Cancer
|
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.
|
-
- HY-135270
-
-
- HY-15378
-
-
- HY-113044
-
-
- HY-12707
-
-
- HY-119943
-
|
PF-06256142
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
|
-
- HY-N6868
-
-
- HY-124733A
-
-
- HY-P1348
-
-
- HY-103178
-
|
MRE3008F20
|
Adenosine Receptor
|
Cancer
|
|
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
|
-
- HY-B1276A
-
-
- HY-14823
-
-
- HY-101370
-
-
- HY-U00036
-
|
Naveglitazar racemate
LY519818 racemate
|
PPAR
|
Metabolic Disease
|
|
Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
|
-
- HY-N0630
-
-
- HY-121885
-
|
LMD-009
|
CCR
|
Metabolic Disease
Endocrinology
|
|
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
|
-
- HY-14171S
-
|
Bexarotene D4
LGD1069 D4
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-14330
-
|
ABT-724
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
|
-
- HY-19733
-
-
- HY-19608
-
-
- HY-N0170
-
-
- HY-12848
-
|
SAG
|
Smo
|
Cancer
|
|
SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-70081A
-
|
Sumanirole maleate
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.
|
-
- HY-135895
-
-
- HY-109137
-
|
Selgantolimod
GS-9688
|
Toll-like Receptor (TLR)
HBV
|
Infection
|
|
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
|
-
- HY-B0154
-
-
- HY-111149A
-
|
PS372424 hydrochloride
|
CXCR
|
Inflammation/Immunology
|
|
PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-12848C
-
|
SAG dihydrochloride
|
Smo
|
Cancer
|
|
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-12848B
-
|
SAG hydrochloride
|
Smo
|
Cancer
|
|
SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG hydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-12288
-
-
- HY-P1279
-
-
- HY-100781A
-
|
L-APB
L-AP 4
|
mGluR
|
Neurological Disease
|
|
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
|
-
- HY-P1295
-
|
Urocortin, human
Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
|
-
- HY-100013A1
-
-
- HY-14558
-
|
Tandospirone
SM-3997
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
|
-
- HY-14289
-
|
Cimetidine
SKF-92334
|
Histamine Receptor
|
Cancer
Endocrinology
|
|
Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.
|
-
- HY-111149
-
|
PS372424
|
CXCR
|
Inflammation/Immunology
|
|
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-P1540
-
-
- HY-117071
-
-
- HY-50760
-
|
L-692585
|
GHSR
|
Endocrinology
|
|
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
|
-
- HY-108525
-
|
Fluorobexarotene
|
RAR/RXR
|
Cancer
|
|
Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.
|
-
- HY-103181
-
-
- HY-12764
-
|
6-OAU
GTPL5846
|
GPR84
|
Inflammation/Immunology
|
|
6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
|
-
- HY-100176
-
-
- HY-19522A
-
|
Seladelpar sodium salt
MBX-8025 sodium salt; RWJ-800025 sodium salt
|
PPAR
|
Metabolic Disease
|
|
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.
|
-
- HY-P1537
-
-
- HY-P1418A
-
|
DPC-AJ1951 TFA
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
DPC-AJ1951 TFA, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
|
-
- HY-P7060
-
|
NT 13
TPPT
|
iGluR
|
Neurological Disease
|
|
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
|
-
- HY-P1132
-
-
- HY-15451
-
|
MDA 19
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.
|
-
- HY-112612A
-
|
RTI-13951-33 hydrochloride
|
Others
|
Neurological Disease
|
|
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.
|
-
- 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-112706
-
|
PF-06747711
|
ROR
|
Inflammation/Immunology
|
|
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity.
|
-
- HY-B0406
-
|
Bethanechol
Carbamyl-β-methylcholine
|
mAChR
|
Neurological Disease
|
|
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-B0406A
-
|
Bethanechol chloride
Carbamyl-β-methylcholine chloride
|
mAChR
|
Neurological Disease
|
|
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-B1675
-
|
Levalbuterol
(R)-Albuterol; (R)-Salbutamol; Levosalbutamol
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.
|
-
- HY-B0471
-
-
- HY-113151
-
-
- HY-100807
-
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.
|
-
- HY-A0261
-
|
Pentagastrin
ICI-50123
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
|
|
Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury.
|
-
- HY-P1279A
-
-
- HY-124401
-
|
BT-13
|
RET
|
Neurological Disease
|
|
BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.
|
-
- HY-N0301
-
|
Thiocolchicoside
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
|
-
- HY-126057S
-
|
(R)-Praziquantel D11
|
Parasite
5-HT Receptor
|
Infection
|
|
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.
|
-
- HY-100300
-
-
- HY-B0982
-
-
- HY-100839
-
|
(RS)-(Tetrazol-5-yl)glycine
D,L-(tetrazol-5-yl)glycine; LY 285265
|
iGluR
|
Neurological Disease
|
|
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice.
|
-
- HY-P1206
-
|
CH 275
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
|
-
- HY-13693
-
-
- HY-B0282
-
-
- HY-15682
-
|
TTNPB
Ro 13-7410; Arotinoid acid; AGN191183
|
RAR/RXR
Autophagy
Apoptosis
|
Cancer
|
|
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
|
-
- HY-18779
-
|
PF-4840154
|
TRP Channel
|
Inflammation/Immunology
|
|
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
|
-
- HY-B1276
-
-
- HY-14153A
-
-
- HY-12597
-
|
Quisqualic acid
L-Quisqualic acid
|
iGluR
mGluR
|
Neurological Disease
|
|
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.
|
-
- HY-N7687
-
|
Caulophyllogenin
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.
|
-
- HY-P1132A
-
-
- HY-P1296
-
|
Urocortin, rat
Urocortin (Rattus norvegicus); Rat urocortin;
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
|
-
- HY-B0225B
-
|
Methyldopa hydrate
L-(-)-α-Methyldopa hydrate; MK-351 hydrate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-16687A
-
-
- HY-117516
-
|
SR10067
|
Others
|
Neurological Disease
|
|
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
|
-
- HY-B0225A
-
|
Methyldopa hydrochloride
L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-B0007
-
|
Baclofen
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA-B receptor (GABABR) agonist. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
|
-
- HY-17609
-
|
Difelikefalin
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
|
-
- HY-P1502
-
|
β-Endorphin, human
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
|
-
- HY-10912
-
|
Fexaramine
|
FXR
Autophagy
|
Others
|
|
Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
|
-
- HY-13580
-
|
Budesonide
|
Glucocorticoid Receptor
|
Cancer
Inflammation/Immunology
|
|
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
|
-
- HY-123268
-
|
Ro 363
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
-
- HY-W013788
-
-
- HY-N0285
-
|
Imperatorin
Ammidin
|
AChE
TRP Channel
|
Neurological Disease
|
|
Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
|
-
- HY-B0225
-
|
Methyldopa
L-(-)-α-Methyldopa; MK-351
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa (L-(-)-α-Methyldopa), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-102091
-
|
(2R,4R)-APDC
|
mGluR
|
Neurological Disease
|
|
(2R,4R)-APDC is a selective group II metabotropic glutamate receptors (mGluRs) agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects.
|
-
- HY-116506
-
|
Bigelovin
|
RAR/RXR
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
|
-
- HY-111455
-
|
LP-211
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-133533
-
-
- HY-N2037
-
|
Higenamine
Norcoclaurine
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine (Norcoclaurine) has anti-apoptotic effects.
|
-
- HY-15293B
-
|
JTV-519 hemifumarate
K201 hemifumarate
|
Calcium Channel
|
Cardiovascular Disease
|
|
JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
|
-
- HY-P1338
-
|
PL-017
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats.
|
-
- HY-B0030
-
|
D-Cycloserine
|
iGluR
Bacterial
Antibiotic
|
Infection
Neurological Disease
|
|
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
|
-
- 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-B0390
-
|
Mestranol
|
Estrogen Receptor/ERR
|
Cancer
Endocrinology
|
|
Mestranol is an inactive prodrug and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders.
|
-
- HY-16687
-
-
- HY-P3061
-
-
- HY-10061
-
|
Lesogaberan
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.
|
-
- HY-13928
-
-
- HY-103244
-
|
CITCO
|
Apoptosis
|
Cancer
|
|
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
|
-
- HY-B0020
-
-
- HY-106993
-
|
Cipralisant
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has the potential for attention-deficit hyperactivity disorder treatment.
|
-
- HY-14442
-
-
- HY-A0158
-
|
Diflorasone
|
Others
|
Inflammation/Immunology
|
|
Diflorasone act as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties. Diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Diflorasone is used for the research of skin diseases such as eczema or psoriasis.
|
-
- HY-N2037A
-
-
- HY-12641
-
|
Pyrantel tartrate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel tartrate, a tetrahydropyrimidine broad-spectrum anthelmintic, and is a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel tartrate can elicit spastic muscle paralysis in parasitic worms. Pyrantel tartrate can be used for the research of astrointestinal nematodes infections.
|
-
- HY-105285
-
-
- HY-B0976
-
|
Fenoterol
Th-1165; Phenoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
|
-
- HY-18978
-
|
GR79236
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.
|
-
- HY-12560A
-
|
PNU-282987
|
nAChR
|
Neurological Disease
|
|
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
|
-
- HY-17606
-
|
Cenerimod
ACT-334441
|
LPL Receptor
|
Inflammation/Immunology
|
|
Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
|
-
- HY-N0092
-
-
- HY-19961
-
|
KIN1408
|
HCV
Influenza Virus
|
Infection
|
|
KIN1408 is an agonist of the RIG-1-like receptor (RLR) pathway and exhibits a broad-spectrum antiviral activity. KIN1408 exhibits activity against HCV, influenza A, dengue virus 2, Ebola, Nipah, and Lassa viruses.
|
-
- HY-109083
-
|
Cilofexor
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
|
-
- HY-107495
-
-
- HY-119243
-
-
- HY-103243
-
|
TCPOBOP
|
Bcl-2 Family
|
Cancer
|
|
TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
|
-
- HY-108523
-
|
LG100754
UVI 2112
|
RAR/RXR
|
Metabolic Disease
|
|
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
|
-
- HY-129658
-
-
- HY-P1294
-
-
- HY-111547
-
|
M1001
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex.
|
-
- HY-P1252
-
-
- HY-110000
-
-
- HY-108699
-
|
TM-N1324
|
GHSR
|
Neurological Disease
Endocrinology
|
|
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn 2+, and 280 nM/180 nM in the absence of Zn 2+ for human/murine GPR39.
|
-
- HY-101310
-
|
SYM 2081
|
iGluR
|
Neurological Disease
|
|
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.
|
-
- HY-15128
-
-
- HY-100608
-
|
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-P1298
-
|
Sauvagine
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-12720A
-
|
Apraclonidine hydrochloride
ALO 2145
|
Others
|
Neurological Disease
|
|
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid.
|
-
- HY-P1338A
-
|
PL-017 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.
|
-
- HY-14728
-
|
Aleglitazar
R1439; RO0728804
|
PPAR
|
Metabolic Disease
|
|
Aleglitazar (R1439;RO0728804) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
|
-
- HY-A0095S
-
|
Flibanserin D4
BIMT-17 D4; BIMT-17BS D4
|
5-HT Receptor
|
Neurological Disease
|
|
Flibanserin D4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM).
|
-
- HY-12585
-
|
AM-4668
|
GPR40
|
Metabolic Disease
|
|
AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.
|
-
- HY-12365
-
|
Namodenoson
CF-102; 2-Cl-IB-MECA
|
Adenosine Receptor
|
Cancer
|
|
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
|
-
- HY-P1252A
-
-
- HY-12640
-
|
Pyrantel pamoate
Pyrantel embonate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel pamoate (Pyrantel embonate), a tetrahydropyrimidine broad-spectrum anthelmintic, and is a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel pamoate can elicit spastic muscle paralysis in parasitic worms. Pyrantel pamoate can be used for the research of astrointestinal nematodes infections.
|
-
- HY-117407
-
|
ALLO-2
|
Smo
|
Cancer
|
|
ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
|
-
- HY-B0180
-
-
- HY-119943A
-
|
(Rac)-PF-06256142
|
Dopamine Receptor
|
Neurological Disease
|
|
(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease.
|
-
- HY-B0180A
-
-
- HY-15293A
-
|
JTV-519 free base
K201 free base
|
Calcium Channel
|
Cardiovascular Disease
|
|
JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
|
-
- HY-110120
-
|
DSR-6434
|
Toll-like Receptor (TLR)
|
Cancer
|
|
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
|
-
- HY-19383
-
|
Ertiprotafib
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-B0180B
-
-
- HY-P1249
-
|
Neuropeptide SF(mouse,rat)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with Ki values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
|
-
- HY-131265
-
-
- HY-136238
-
-
- HY-13665
-
|
Leuprolide Acetate
Leuprorelin acetate
|
GNRH Receptor
|
Endocrinology
Cancer
|
|
Leuprolide Acetate (Leuprorelin acetate) is an analogue of gonadotrophin-releasing hormone (GnRH), acts as a GnRH receptor agonist. Leuprolide Acetate can be used for the research of prostate cancer, endometriosis, uterine fibroids, central precocious puberty, multiple sclerosis. Leuprolide Acetate improves experimental autoimmune encephalomyelitis in rat model.
|
-
- HY-B0072
-
-
- HY-129105
-
