Search Result
Results for "Antifolate Agonists" in MCE Product Catalog:
1323
Inhibitors & Agonists
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-19095
-
|
TNP-351
|
Antifolate
|
Cancer
|
|
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
|
-
- HY-130569
-
|
7-Hydroxymethotrexate
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- HY-10446
-
|
Pralatrexate
|
Antifolate
Apoptosis
|
Cancer
|
|
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
|
-
- 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-15394
-
-
- HY-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- 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-N2548
-
-
- 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-137773
-
|
N-Methyl pemetrexed
|
Others
|
Cancer
|
|
N-Methyl pemetrexed is an impurity of Pemetrexed. Pemetrexed is an antifolate cytotoxic agent that can be used for the research of cancer.
|
-
- HY-14523
-
|
LY 254155
|
Antifolate
|
Cancer
|
|
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
|
-
- 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-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-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-13781
-
|
Pemetrexed disodium hemipenta hydrate
LY231514 disodium hemipenta hydrate
|
Antifolate
Autophagy
Apoptosis
|
Cancer
|
|
Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
-
- 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-10820
-
|
Pemetrexed
LY231514
|
Antifolate
Autophagy
|
Cancer
|
|
Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
-
- 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.
|
-
- HY-133112
-
-
- HY-10820A
-
|
Pemetrexed disodium
LY231514 disodium
|
Antifolate
Autophagy
Apoptosis
|
Cancer
|
|
Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
|
-
- HY-133887
-
-
- HY-133624
-
|
1,1,3-Tribromoacetone
|
Others
|
Cancer
|
|
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- 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-107981
-
|
LSN 3213128
|
Antifolate
|
Cancer
|
|
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
|
-
- 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-129441
-
-
- 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-14519
-
|
Methotrexate
Amethopterin; CL14377; WR19039
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- 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-14519A
-
|
Methotrexate disodium
Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- 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-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-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-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-B2245
-
-
- HY-107399
-
-
- HY-17354A
-
-
- HY-17354
-
-
- HY-P0236A
-
-
- HY-110304
-
-
- HY-136435
-
-
- HY-114400
-
-
- 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-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-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-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-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-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.
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-
- HY-N0808
-
-
- HY-A0008
-
-
- HY-B0316
-
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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-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-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-18936
-
-
- 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-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
-
|
Clomethiazole
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
|
Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
|
-
- HY-P1294A
-
-
- HY-12498
-
|
GV-58
|
Calcium Channel
|
Neurological Disease
|
|
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
|
-
- HY-15483
-
-
- HY-133024
-
|
Flumexadol
|
5-HT Receptor
|
Neurological Disease
|
|
Flumexadol is an orally active non-narcotic analgesic. Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor.
|
-
- HY-121653
-
|
Flesinoxan
|
5-HT Receptor
|
Neurological Disease
|
|
Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.
|
-
- HY-P1319
-
|
Nociceptin(1-7)
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
|
-
- HY-18282
-
|
AZ876
|
LXR
|
Cancer
|
|
AZ876 is a potent and high-affinity LXR agonist. AZ876 displays 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.
|
-
- HY-103551A
-
|
LY 541850
|
mGluR
|
Neurological Disease
|
|
LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
|
-
- HY-107413
-
|
SR11237
BMS-649
|
RAR/RXR
|
Cancer
|
|
SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.
|
-
- HY-15296
-
-
- HY-15778A
-
-
- HY-108015
-
|
RO5263397
|
Others
|
Neurological Disease
|
|
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.
|
-
- HY-136657
-
|
SC-43
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
|
-
- HY-100488
-
|
Bay 59-3074
|
Cannabinoid Receptor
|
Cancer
|
|
Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
|
-
- HY-110318
-
|
VUF11207 fumarate
|
CXCR
|
Cancer
|
|
VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
|
-
- HY-12023
-
|
GTx-007
S-4
|
Androgen Receptor
|
Cancer
|
|
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.
|
-
- HY-15701B
-
|
ADH-503
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-14903
-
|
Ulimorelin
TZP-101
|
GHSR
Adrenergic Receptor
|
Metabolic Disease
|
|
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
|
-
- HY-P1214
-
-
- HY-P1298A
-
|
Sauvagine TFA
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-P1341
-
-
- HY-115682
-
|
(S)-ZINC-3573
|
Others
|
Others
|
|
(S)-ZINC-3573, an inactive enantiomer of ZINC-3573, is a negative control for (R)-ZINC-3573. (R)-ZINC-3573 is a selective MRGPRX2 agonist. (S)-ZINC-3573 displays no activity at MRGPRX2 at concentrations below 100 μM.
|
-
- HY-100689
-
|
Propyl pyrazole triol
PPT
|
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
|
-
- HY-P1249A
-
-
- HY-105296
-
|
Blarcamesine
AVex-73; AE-37
|
Sigma Receptor
mAChR
|
|
|
Blarcamesine (AVex-73;AE-37) is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
|
-
- HY-16995
-
-
- HY-109035
-
|
Inarigivir soproxil
SB9200
|
HCV
|
Infection
|
|
Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.
|
-
- HY-15780
-
-
- HY-13221
-
-
- HY-B0976A
-
|
Fenoterol hydrobromide
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
|
-
- HY-11062
-
|
Icilin
AG-3-5
|
TRP Channel
|
Cancer
Neurological Disease
|
|
Icilin (AG-3-5) is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. Icilin activated currents only in wild type TRPM8 and in the presence of Ca 2+. Icilin can induce G1 arrest in prostate cancer cells.
|
-
- HY-19360
-
|
Sulprostone
SHB 286; CP-34089; ZK-57671
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Sulprostone (SHB 286) is a potent and selective EP3 receptor agonist. Sulprostone (SHB 286) is a prostaglandin E2 (PGE2) analogue and has antiulcer and nonsteroidal abortifacient effects. Sulprostone has potential for the research of pregnancy termination and hemorrhages during delivery.
|
-
- HY-12956
-
-
- HY-N7032
-
-
- HY-10349
-
|
WAY-100635
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 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 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
|
-
- HY-120528A
-
-
- HY-P1091
-
|
Hemopressin (human, mouse)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
|
-
- HY-103186
-
-
- HY-12066
-
-
- HY-13225
-
|
Rivanicline oxalate
RJR-2403 oxalate; (E)-Metanicotine oxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-B0637
-
|
Bezafibrate
BM15075
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-107514
-
|
(RS)-PPG
|
mGluR
|
Neurological Disease
|
|
(RS)-PPG is a potent and selective agonist for group III mGluRs. The EC50s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.
|
-
- HY-13225B
-
|
Rivanicline hemioxalate
RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-124136
-
|
WYC-209
|
RAR/RXR
Apoptosis
Autophagy
|
Cancer
|
|
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.
|
-
- HY-B0372A
-
|
Bromhexine hydrochloride
|
SARS-CoV
Autophagy
HIV
|
Metabolic Disease
|
|
Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
|
-
- HY-B1696A
-
|
Methyldopate hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
|
-
- HY-P1256
-
|
JMV 449
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.5 nM in binding to mouse brain membranes and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
|
-
- HY-P2454
-
|
CSP1
|
Bacterial
|
Infection
|
|
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.
|
-
- HY-P3057
-
|
[D-Trp11]-Neurotensin
|
Neurotensin Receptor
|
Neurological Disease
|
|
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension.
|
-
- HY-101173
-
|
Imetit dihydrobromide
VUF 8325 dihydrobromide; SKF 91105 dihydrobromide
|
Histamine Receptor
|
Neurological Disease
|
|
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM).
|
-
- HY-P1316
-
|
Ac-RYYRWK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-19358A
-
|
2-Methyl-5-HT hydrochloride
2-Methyl-5-hydroxytryptamine hydrochloride; 2-Methylserotonin hydrochloride; 2-Me-HT hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine hydrochloride) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT hydrochloride is shown to display anti-depressive-like effects.
|
-
- HY-106660
-
|
BP 897
|
Dopamine Receptor
|
Neurological Disease
|
|
BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 µM, respectively).
|
-
- HY-100999
-
-
- HY-15701A
-
|
(Z)-Leukadherin-1
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-P1341A
-
-
- HY-135750
-
|
VAF347
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
|
-
- HY-15129
-
|
O-Phospho-L-serine
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
|
-
- HY-B1557
-
|
Betazole
Ametazole
|
Histamine Receptor
|
Metabolic Disease
|
|
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity.
|
-
- HY-19231
-
|
DPI-3290
Org 41793
|
Opioid Receptor
|
Neurological Disease
|
|
DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.
|
-
- HY-P1316A
-
|
Ac-RYYRWK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-19358
-
|
2-Methyl-5-HT
2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.
|
-
- HY-P1319A
-
|
Nociceptin(1-7) TFA
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
|
-
- HY-116637
-
|
Tetrahydromagnolol
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
|
-
- HY-108741
-
|
Plecanatide
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-12752
-
|
Alimemazine
Trimeprazine
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays sedative, antiserotonin, antispasmodic, and antiemetic properties.
|
-
- HY-119104
-
|
AZD1940
|
Cannabinoid Receptor
|
Neurological Disease
|
|
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
|
-
- HY-P1214A
-
-
- HY-131180
-
|
BMS-986235
LAR-1219
|
Others
|
Cardiovascular Disease
|
|
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
|
-
- HY-19358B
-
|
2-Methyl-5-HT maleate
2-Methyl-5-hydroxytryptamine maleate; 2-Methylserotonin maleate; 2-Me-HT maleate
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT maleate is shown to display anti-depressive-like effects.
|
-
- HY-103697A
-
|
Gardiquimod diTFA
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-101037
-
|
Sarcosine
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (N-Methylglycine; Sarcosin), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor an N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.
|
-
- HY-119744
-
|
BAY 38-7271
|
Cannabinoid Receptor
|
Neurological Disease
|
|
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
|
-
- HY-10046
-
-
- HY-14611
-
|
3,3'-Difluorobenzaldazine
DFB
|
mGluR
|
Neurological Disease
|
|
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range.
|
-
- HY-B0032A
-
-
- HY-17034A
-
|
Dexmedetomidine hydrochloride
(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
|
-
- HY-B0032
-
|
Lurasidone Hydrochloride
SM-13496 Hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
|
-
- HY-B1557A
-
|
Betazole dihydrochloride
Ametazole dihydrochloride
|
Histamine Receptor
|
Metabolic Disease
|
|
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.
|
-
- HY-13956S
-
|
Pioglitazone D4
U 72107 D4
|
PPAR
Ferroptosis
|
Cancer
Metabolic Disease
|
|
Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. 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-W020468
-
|
Linopirdine
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
|
-
- HY-112813
-
|
TUG-1375
|
Others
|
Metabolic Disease
|
|
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
|
-
- HY-P0227
-
|
SHU 9119
|
Melanocortin Receptor
|
Metabolic Disease
|
|
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
|
-
- HY-113854
-
-
- HY-B1810
-
|
Tulobuterol
C-78 free base
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength.
|
-
- HY-P1112
-
-
- HY-100450
-
-
- HY-12150
-
|
CCMI
|
nAChR
|
Neurological Disease
|
|
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
|
-
- HY-101176
-
|
2-Iodomelatonin
|
Melatonin Receptor
|
Cancer
|
|
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
|
-
- HY-113008A
-
|
cis-Urocanic acid
(Z)-Urocanic acid; cis-UCA
|
5-HT Receptor
|
Inflammation/Immunology
|
|
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
|
-
- HY-13306
-
|
Pyrintegrin
|
Integrin
|
Metabolic Disease
|
|
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
|
-
- HY-W010907
-
|
Pamoic acid disodium
|
ERK
|
Neurological Disease
|
|
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
|
-
- HY-128865
-
|
BPR1M97
|
Opioid Receptor
|
Neurological Disease
|
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
|
-
- HY-101854
-
-
- HY-B1322A
-
-
- HY-100804
-
|
L-Cysteinesulfinic acid
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
|
-
- HY-110173
-
|
TC-G 1005
|
GPCR19
|
Metabolic Disease
|
|
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
|
-
- HY-14813
-
|
Cutamesine
SA4503; AGY 94806
|
Sigma Receptor
|
Neurological Disease
|
|
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
|
-
- HY-P1112A
-
-
- HY-P1090
-
|
Hemopressin(rat)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
|
-
- HY-W017230
-
|
L-Cysteinesulfinic acid monohydrate
|
mGluR
|
Neurological Disease
|
|
L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
|
-
- HY-111793
-
|
NUCC-390
|
CXCR
|
Neurological Disease
|
|
NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.
|
-
- HY-P1091A
-
|
Hemopressin(human, mouse) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-B0061
-
|
Tandospirone citrate
SM-3997 citrate
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
|
-
- HY-76772
-
|
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- HY-111793A
-
|
NUCC-390 dihydrochloride
|
CXCR
|
Neurological Disease
|
|
NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.
|
-
- HY-P1423A
-
|
BA 1 TFA
|
Bombesin Receptor
|
Cancer
Metabolic Disease
|
|
BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
|
-
- HY-P1072
-
|
PHM-27 (human)
|
CGRP Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
|
-
- HY-100808
-
|
(R)-Serine
|
iGluR
Endogenous Metabolite
|
Others
|
|
(R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. (R)-Serine has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
|
-
- HY-12956A
-
|
Dinoprost tromethamine salt
Prostaglandin F2α tromethamine salt; PGF2α THAM; Prostaglandin F2α THAM
|
Prostaglandin Receptor
Endogenous Metabolite
Autophagy
Apoptosis
|
Endocrinology
|
|
Dinoprost tromethamine salt (Prostaglandin F2α tromethamine salt) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost tromethamine salt is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost tromethamine salt plays a key role in the onset and progression of labour.
|
-
- HY-110279
-
|
Ogerin
|
Others
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
|
-
- HY-14262
-
|
Vilazodone
EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
|
-
- HY-117066
-
|
CL075
3M002
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
|
-
- HY-P1423
-
|
BA 1
|
Bombesin Receptor
|
Cancer
Metabolic Disease
|
|
BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
|
-
- HY-108497
-
|
L-803087
|
Somatostatin Receptor
|
Cancer
Neurological Disease
|
|
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
|
-
- HY-10473
-
|
Eprotirome
KB2115
|
Thyroid Hormone Receptor
|
Endocrinology
Metabolic Disease
|
|
Eprotirome (KB2115) is a liver-selective thyroid hormone receptor (TR) agonist. KB2115 has modestly higher affinity for TRβ than for TRα. Eprotirome reduces low-density lipoprotein (LDL) cholesterol concentrations. Eprotirome can be used for dyslipidemias and obesity research.
|
-
- HY-101698
-
|
Alniditan
Alnitidan
|
5-HT Receptor
|
Neurological Disease
|
|
Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
|
-
- HY-14539
-
|
Clozapine
HF 1854
|
Dopamine Receptor
mAChR
|
Neurological Disease
|
|
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
|
-
- HY-134130
-
|
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-70020B
-
|
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-126351
-
|
PROTAC ERRα ligand 2
|
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
|
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- HY-12980
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- HY-10964
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Vadimezan
DMXAA; ASA-404
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STING
IFNAR
Influenza Virus
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Cancer
Infection
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Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.
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- HY-129851
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NTP42
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Prostaglandin Receptor
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Cardiovascular Disease
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NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
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- HY-120006A
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(rel)-AR234960
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ERK
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Cardiovascular Disease
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(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
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- HY-130120
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HWL-088
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GPR40
PPAR
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Metabolic Disease
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HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
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- HY-14151
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Prucalopride
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5-HT Receptor
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Neurological Disease
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Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.
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- HY-12598
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(S)-3,5-DHPG
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mGluR
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Neurological Disease
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(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.
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- HY-42110
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Deschloroclozapine
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mAChR
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Neurological Disease
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Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [ 3H]quinuclidinyl benzilate (QNB) binding to hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications.
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- HY-B1816
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- HY-15688
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8-Hydroxy-DPAT hydrobromide
8-OH-DPAT hydrobromide
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5-HT Receptor
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Neurological Disease
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8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
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- HY-10232
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THIP
Gaboxadol
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GABA Receptor
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Neurological Disease
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THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
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- HY-113209
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8-Isoprostaglandin F2α
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Endogenous Metabolite
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Others
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8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
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- HY-15536
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Cebranopadol
GRT6005
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Opioid Receptor
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Neurological Disease
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Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
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- HY-B1532
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Anabasine
(S)-Anabasine; (+)-Anabasine
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nAChR
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Neurological Disease
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Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM).
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- HY-W014928
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Anabasine hydrochloride
(S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride
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nAChR
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Neurological Disease
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Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM).
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- HY-19838
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JNJ-63533054
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GPR139
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Neurological Disease
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JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
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- HY-136363
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MDR-652
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TRP Channel
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Neurological Disease
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MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
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- HY-134189A
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- HY-104037
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Cintirorgon
LYC-55716
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ROR
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Cancer
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Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
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- HY-124071
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ACT-389949
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Others
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Inflammation/Immunology
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ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders.
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- HY-108795A
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Albiglutide TFA
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Glucagon Receptor
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Metabolic Disease
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Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus (T2DM). Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin.
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- HY-N3940
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Gelsevirine
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Others
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Cancer
Neurological Disease
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Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively.
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- HY-100256
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Trifarotene
CD5789
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RAR/RXR
Autophagy
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Inflammation/Immunology
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Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively.
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- HY-134189
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EST73502
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
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- HY-14539S
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Clozapine D8
HF 1854 D8
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Dopamine Receptor
mAChR
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Neurological Disease
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Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
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- HY-70020
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Cevimeline
AF102B
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mAChR
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Neurological Disease
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Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
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- HY-P1090A
