Search Result
Results for "Angiotensin Receptor Modulators" in MCE Product Catalog:
3613
Inhibitors & Agonists
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-P3138
-
|
(Sar1)-Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a Kd of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes.
|
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- HY-113035
-
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- HY-P0108
-
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- HY-113035A
-
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- HY-13948
-
|
Angiotensin II human
Angiotensin II; Ang II; DRVYIHPF
|
Angiotensin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
|
-
- HY-13948A
-
|
Angiotensin II human acetate
Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate
|
Angiotensin Receptor
Apoptosis
|
Cancer
Endocrinology
Cardiovascular Disease
|
|
Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis.
|
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- HY-P1515
-
-
- HY-P1515A
-
-
- HY-12403
-
|
Angiotensin (1-7)
Ang-(1-7)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cardiovascular Disease
Endocrinology
|
|
Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
|
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- HY-P1540
-
-
- HY-P1792
-
|
Angiotensin II (1-4), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
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- HY-P1769
-
|
Angiotensin II (5-8), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
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Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
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- HY-P1792A
-
|
Angiotensin II (1-4), human TFA
|
Angiotensin Receptor
|
Endocrinology
Metabolic Disease
|
|
Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
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- HY-P1839
-
|
Angiotensin I/II (1-5)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-5 is a peptide that contains the amino acids 1-5, which is converted from Angiotensin I/II. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
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- HY-P1829
-
|
Angiotensin I/II (1-6)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
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Angiotensin I/II 1-6 contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
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- HY-50900
-
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- HY-131278
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- HY-136275
-
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AMPA receptor modulator-2
|
iGluR
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Others
|
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AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor. pIC50 = -lgIC50.
|
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- HY-10018
-
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- HY-114953
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- HY-15618
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- HY-10933
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CX516
BDP 12
|
iGluR
|
Neurological Disease
|
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CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
|
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- HY-U00429
-
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- HY-110201
-
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Estrogen receptor modulator 1
|
Estrogen Receptor/ERR
|
Cancer
|
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Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
|
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- HY-P1564
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- HY-U00420
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- HY-U00339
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- HY-100113
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- HY-133021
-
|
Arazine
N-Acetyl-S-farnesyl-L-cysteine
|
Others
|
Inflammation/Immunology
|
|
Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
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- HY-112699
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- HY-P0205B
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- HY-P2563
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- HY-109058
-
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Firibastat
QGC001; RB150
|
Aminopeptidase
|
Cardiovascular Disease
|
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Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
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- HY-116330A
-
|
Hyperforin dicyclohexylammonium salt
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
|
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- HY-18204A
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- HY-129946
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- HY-134661
-
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GPR6 modulator 1
|
Others
|
Neurological Disease
|
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GPR6 modulator 1 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. GPR6 modulator 1 has the potential for a variety of neurological and psychiatric disorders, including Parkinson's disease.
|
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- HY-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
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GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
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- HY-P2518
-
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- HY-B0384
-
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- HY-P2519
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- HY-P1486
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- HY-117959
-
|
TAK-615
|
LPL Receptor
|
Inflammation/Immunology
|
|
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
|
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- HY-A0036
-
|
Bazedoxifene acetate
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
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- HY-A0031
-
|
Bazedoxifene
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
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- HY-A0031A
-
|
Bazedoxifene hydrochloride
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
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Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
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- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
|
Neurological Disease
|
|
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
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- HY-12765
-
|
Losartan Carboxylic Acid
E-3174; EXP-3174
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
|
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- 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.
|
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- HY-17512
-
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- HY-B1494
-
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- 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.
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- HY-101058
-
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- HY-15778
-
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- HY-113920A
-
|
Azumolene
EU4093 free base
|
Calcium Channel
|
Metabolic Disease
|
|
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
|
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- HY-P0080
-
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- HY-101574
-
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- HY-17446
-
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- HY-108896
-
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- HY-P0080A
-
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- HY-17512S
-
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- HY-128128
-
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ASN04421891
|
Others
|
Neurological Disease
|
|
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
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- HY-13757AS
-
|
Tamoxifen-d5
ICI 47699-d5; (Z)-Tamoxifen-d5; trans-Tamoxifen-d5
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
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- HY-128575
-
|
BNC375
|
nAChR
|
Neurological Disease
|
|
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-drug like properties and clinical candidate potential.
.
|
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- HY-U00245
-
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- HY-U00202
-
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- HY-111052
-
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AZD7325
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
Neurological Disease
|
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AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
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- HY-102093
-
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- HY-13017S
-
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Ivacaftor-D9
CTP-656
|
CFTR
|
Cancer
|
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Ivacaftor-D9 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research.
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- HY-17512A
-
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- HY-A0250
-
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- HY-B0205
-
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- HY-100292
-
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- HY-108250
-
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(R)-Bicalutamide
|
Androgen Receptor
|
Cancer
|
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(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
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- HY-14234
-
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- HY-14612
-
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CPPHA
|
mGluR
|
Neurological Disease
|
|
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.
|
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- 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.
|
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- HY-19732
-
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- HY-101618
-
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- HY-110278
-
|
ADX71743
|
mGluR
|
Neurological Disease
|
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
|
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- HY-113313
-
|
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
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- HY-P0297
-
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- HY-101706
-
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- HY-U00188
-
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- HY-10259
-
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- HY-10259A
-
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- HY-10036
-
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- HY-50159
-
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- HY-50158
-
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- HY-114348
-
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N,N'-Diacetyl-L-cystine
DiNAC; (Ac-Cys-OH)2
|
Others
|
Cardiovascular Disease
|
|
N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits.
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- HY-19630
-
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ML289
VU0463597
|
mGluR
|
Neurological Disease
|
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ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
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- HY-17005
-
-
- HY-17505
-
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- HY-124906
-
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JAMI1001A
|
iGluR
|
Neurological Disease
|
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JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
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- HY-107457
-
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AZD-8529
|
mGluR
|
Neurological Disease
|
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AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
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- HY-P0283
-
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- HY-107457A
-
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AZD-8529 mesylate
|
mGluR
|
Neurological Disease
|
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AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
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- HY-131974
-
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- HY-112189
-
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- HY-128781
-
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- HY-124600
-
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NVR 3-778
|
HBV
|
Infection
|
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NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
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- HY-16734A
-
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Amiselimod hydrochloride
MT-1303 hydrochloride
|
LPL Receptor
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Cancer
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Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
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- HY-105272A
-
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- HY-105272
-
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Loreclezole
R 72063
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GABA Receptor
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Neurological Disease
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Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
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- HY-B1264
-
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Celiprolol hydrochloride
|
Adrenergic Receptor
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Cardiovascular Disease
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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.
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- HY-B0202
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- HY-14914
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- HY-B0780
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- HY-19191
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- HY-50713
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- HY-P1840
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- HY-135671
-
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- HY-112154
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- HY-B0205S
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- HY-14569
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CDPPB
|
mGluR
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Neurological Disease
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CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
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- HY-13757A
-
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Tamoxifen
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
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Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis.
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- HY-12439
-
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ML380
|
mAChR
|
Neurological Disease
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ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
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- HY-135363
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- HY-18204
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- HY-13757
-
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Tamoxifen Citrate
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
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Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.
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- HY-N2371
-
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- HY-112451
-
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- HY-B0202S
-
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- HY-136922
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- HY-P1840A
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- HY-133486
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- HY-13955
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- HY-103668A
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- HY-16950
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- HY-B0463
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- HY-101216
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- HY-16423
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- HY-18076
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- HY-17004
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- HY-137093
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- HY-133123
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- HY-131264
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- HY-12405
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- HY-12765S
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- HY-17621
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- HY-19214
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- HY-17458
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- HY-A0038
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- HY-114530
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- HY-100186
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- HY-101845
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FITM
|
mGluR
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Cancer
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FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
|
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- HY-U00387
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- HY-75502
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- HY-101583
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- HY-114017
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- HY-136645
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- HY-138501
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- HY-14736
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- HY-131277
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- HY-130992
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- HY-114025
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- HY-106182
-
-
- HY-U00360
-
-
- HY-100366
-
-
- HY-15834A
-
-
- HY-112679
-
-
- HY-133555
-
-
- HY-111453
-
-
- HY-U00178
-
-
- HY-112185
-
-
- HY-136459
-
|
NMDA receptor antagonist 2
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
|
-
- HY-P1308
-
-
- HY-135482
-
|
GABAA receptor agent 2 TFA
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
|
-
- HY-106199
-
-
- 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-131276
-
-
- HY-14914S
-
|
Azilsartan D5
TAK-536 D5
|
Angiotensin Receptor
|
Others
|
|
Azilsartan D5 (TAK-536 D5) is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
|
-
- HY-129657
-
|
GLP-1 receptor agonist 4
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.
|
-
- HY-10937
-
-
- HY-109073
-
-
- HY-17004S
-
|
Olmesartan D4
RNH-6270 D4
|
Angiotensin Receptor
|
Others
|
|
Olmesartan D4 (RNH-6270 D4) is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
|
-
- HY-133775
-
-
- HY-131279
-
|
Olmesartan ethyl ester
|
Others
|
Others
|
|
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study.
|
-
- HY-125819
-
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-P0079
-
-
- HY-18102A
-
-
- HY-13724B
-
-
- HY-11027
-
-
- HY-10932
-
-
- HY-119687
-
|
Bifenazate
|
GABA Receptor
|
Infection
|
|
Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor.
|
-
- HY-12509
-
|
PEPA
|
iGluR
|
Neurological Disease
|
|
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
|
-
- HY-P1276
-
-
- HY-100348
-
|
EPI-001
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
|
-
- HY-50162
-
|
GPR120 modulator 1
|
GPR120
|
Metabolic Disease
|
|
GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
|
-
- HY-50172
-
|
GPR120 modulator 2
|
GPR120
|
Metabolic Disease
|
|
GPR120 modulator 2 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F13. GPR120 modulator 2 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
|
-
- HY-111669
-
-
- HY-125821
-
|
Sigma-1 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
|
-
- HY-A0230A
-
|
Spirapril hydrochloride
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- 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-125820
-
-
- HY-U00321
-
-
- HY-129357
-
-
- HY-18204S
-
-
- HY-18162
-
-
- HY-14383
-
-
- HY-125976
-
|
ML233
|
Others
|
Cardiovascular Disease
|
|
ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM).
|
-
- HY-P3108
-
-
- HY-P1276A
-
-
- HY-129656
-
-
- HY-14229
-
-
- HY-14774
-
|
Monepantel
AAD1566
|
nAChR
|
Cancer
|
|
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-109046
-
-
- HY-P1308A
-
-
- HY-108584
-
|
Flindokalner
BMS-204352
|
Potassium Channel
|
Neurological Disease
|
|
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
|
-
- HY-P0318
-
-
- HY-P1758
-
-
- HY-N7247
-
|
Thiochrome
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
|
-
- HY-U00382
-
-
- HY-P1536
-
-
- HY-17030
-
-
- HY-16950B
-
-
- HY-14419
-
-
- HY-19947
-
|
PF-06291874
Glucagon Receptor antagonists-4
|
Glucagon Receptor
|
Metabolic Disease
|
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
|
-
- HY-19320
-
-
- HY-126293
-
|
Apelin agonist 1
|
Others
|
Cardiovascular Disease
|
|
Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0.
|
-
- HY-B2121
-
-
- 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-119941
-
-
- HY-19872
-
-
- HY-102024
-
-
- HY-114412A
-
-
- HY-101704
-
-
- HY-N2096
-
|
Kavain
|
GABA Receptor
|
Neurological Disease
|
|
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
|
-
- HY-N4157
-
-
- HY-14959
-
|
Ulipristal
CDB-3236; Deacetyl CDB-2914
|
Progesterone Receptor
|
Cancer
Endocrinology
|
|
Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
|
-
- HY-W001692
-
-
- HY-18654
-
|
ADX88178
|
mGluR
|
Neurological Disease
|
|
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
|
-
- HY-12157
-
|
VU 0238429
|
mAChR
|
Others
|
|
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
|
-
- HY-101746
-
|
GSK376501A
|
PPAR
|
Metabolic Disease
|
|
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
|
-
- HY-114412
-
-
- HY-101681
-
-
- HY-13288
-
-
- HY-15748
-
|
JNJ-40411813
ADX-71149
|
mGluR
|
Neurological Disease
|
|
JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
|
-
- HY-U00366
-
-
- HY-112426
-
-
- 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-110303
-
-
- HY-B1510S
-
-
- HY-108321
-
-
- HY-B0331
-
-
- HY-U00041
-
-
- HY-13236
-
-
- HY-16951
-
|
VU-1545
|
mGluR
|
Neurological Disease
|
|
VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM.
|
-
- HY-112814
-
|
VU6001376
|
mGluR
|
Neurological Disease
|
|
VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
|
-
- HY-116896
-
|
LY117018
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
|
-
- HY-100409
-
|
PHCCC
|
mGluR
|
Cancer
|
|
PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
|
-
- HY-B0235
-
|
Trichlormethiazide
|
Others
|
Metabolic Disease
|
|
Trichlormethiazide is an orally active thiazide diuretic, antihypertensive effect. Trichlormethiazide increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model.
|
-
- HY-B0655
-
-
- HY-P3137
-
|
TRV056
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-P3136
-
|
TRV055
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-19371
-
|
Lorediplon
|
GABA Receptor
|
Neurological Disease
|
|
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
|
-
- HY-114403
-
|
VU6012962
|
mGluR
|
Neurological Disease
|
|
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
|
-
- HY-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-13277
-
-
- HY-124622
-
-
- HY-116463
-
-
- HY-N3755
-
|
Dihydroresveratrol
|
Estrogen Receptor/ERR
|
Cancer
|
|
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
|
-
- HY-P1818
-
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-135270
-
-
- HY-P1415
-
|
Norleual
|
c-Met/HGFR
|
|
|
Norleual is an angiotensin IV analog. Norleual is a highly potent HGF/c-MET inhibitor (IC50=3 pM). Norleual inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Norleual also is an AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic.
|
-
- HY-112209
-
|
VU0467154
|
mAChR
|
Neurological Disease
|
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
|
-
- HY-B0723
-
|
Ospemifene
FC-1271a
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
|
-
- HY-12508
-
|
CMPDA
|
iGluR
|
Neurological Disease
|
|
CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
|
-
- HY-P0143
-
-
- HY-B0279
-
-
- HY-U00074
-
-
- HY-107337
-
-
- 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-101363
-
|
1-BCP
Piperonylic acid piperidide
|
iGluR
|
Neurological Disease
|
|
1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
|
-
- HY-111498A
-
-
- HY-135329
-
|
Solifenacin D5 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-P1329
-
-
- HY-135585
-
|
LY88074
|
Others
|
Endocrinology
|
|
LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
|
-
- HY-P1329A
-
-
- HY-B0093
-
-
- HY-B1451
-
-
- HY-B0331A
-
-
- HY-A0043A
-
-
- HY-B0093A
-
-
- HY-A0043
-
-
- HY-18102
-
|
GLPG0492
|
Androgen Receptor
|
Others
|
|
GLPG0492 is a non-steroidal selective androgen receptor modulator (potency 12 nM). GLPG0492 has the potential for the research of musculo-skeletal diseases such as sarcopenia and cachexia.
|
-
- HY-N0549
-
-
- HY-P1335
-
|
CTAP
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-107339
-
|
Deserpidine
Harmonyl
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
Neurological Disease
|
|
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.
|
-
- HY-50889
-
-
- HY-103407A
-
-
- HY-P1335A
-
|
CTAP TFA
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-N0050
-
|
Allomatrine
(+)-Allomatrine
|
Others
|
Neurological Disease
|
|
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
|
-
- HY-100658
-
|
Didesmethyl cariprazine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
|
-
- HY-110285
-
|
ML382
|
Others
|
Neurological Disease
|
|
ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
|
-
- HY-103306
-
|
Ryanodine
|
Others
|
Neurological Disease
|
|
Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
|
-
- HY-106446
-
-
- HY-B0231
-
-
- HY-B0477
-
-
- HY-101348
-
-
- HY-B0098S
-
-
- HY-118342
-
|
PQCA
|
mAChR
|
Neurological Disease
|
|
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
|
-
- HY-103040
-
|
Zuranolone
|
GABA Receptor
|
Neurological Disease
|
|
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
|
-
- HY-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-107498
-
|
GNE-8324
|
iGluR
|
Neurological Disease
|
|
GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons.
|
-
- HY-15393
-
|
VU 0357121
|
mGluR
|
Neurological Disease
|
|
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
|
-
- HY-12149
-
|
A-867744
|
nAChR
Autophagy
|
Neurological Disease
|
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
|
-
- HY-135419
-
-
- HY-107395
-
-
- HY-P1488
-
-
- 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-N6905
-
-
- HY-100450
-
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-131941
-
|
SJM-3
|
GABA Receptor
|
Neurological Disease
|
|
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.
|
-
- HY-112256
-
-
- HY-10167A
-
|
Tecalcet Hydrochloride
R-568 hydrochloride
|
CaSR
|
Others
|
|
Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
|
-
- HY-129995A
-
-
- HY-138040
-
-
- 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-128113
-
-
- HY-B0382
-
-
- HY-B0331AS
-
-
- HY-A0116S
-
-
- HY-101577
-
-
- HY-P1167
-
-
- HY-19845A
-
-
- HY-128770
-
-
- HY-108703
-
|
Foliglurax
PXT002331
|
mGluR
|
Neurological Disease
|
|
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
|
-
- HY-108243
-
-
- HY-10863
-
-
- HY-13738A
-
|
Raloxifene hydrochloride
Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
|
-
- HY-106901A
-
|
Asoxime dichloride
HI-6
|
nAChR
|
Neurological Disease
|
|
Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
|
-
- HY-50754
-
-
- HY-10822A
-
|
ONX 0801 trisodium
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
|
-
- HY-18206
-
-
- HY-U00135
-
-
- HY-16950A
-
-
- HY-113320
-
|
Etiocholanolone
5β-Androsterone
|
GABA Receptor
|
Neurological Disease
|
|
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
|
-
- HY-B0311A
-
|
Carbidopa monohydrate
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-B0311
-
|
Carbidopa
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-108710
-
|
VU0650786
|
mGluR
|
Neurological Disease
|
|
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
|
-
- HY-111996
-
-
- HY-135588
-
-
- HY-15706
-
-
- HY-119802
-
-
- HY-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-15404
-
|
Darusentan
Lu-135252
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM.
|
-
- HY-119706
-
|
Barbadin
|
Others
|
Others
|
|
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.
|
-
- HY-108703A
-
|
Foliglurax monohydrochloride
PXT002331 (monohydrochloride)
|
mGluR
|
Neurological Disease
|
|
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
|
-
- HY-12324
-
|
SB269652
|
Dopamine Receptor
|
Neurological Disease
|
|
SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
|
-
- HY-124867
-
|
D3-βArr
|
TSH Receptor
|
Endocrinology
|
|
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
|
-
- HY-13738
-
|
Raloxifene
Keoxifene; LY156758 free base; LY139481
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
|
-
- HY-135891
-
|
AZD2423
|
CCR
|
Neurological Disease
|
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-W040146
-
-
- HY-18200
-
|
Atopaxar
E5555; ER-172594-00
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
|
-
- HY-101299A
-
|
Dihydrexidine
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.
|
-
- HY-101299B
-
|
Dihydrexidine hydrochloride
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.
|
-
- HY-120012
-
-
- 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-16508
-
|
Ulipristal acetate
CDB-2914
|
Progesterone Receptor
Autophagy
|
Endocrinology
Cancer
|
|
Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
|
-
- HY-15731
-
-
- HY-W011100
-
-
- HY-B0378A
-
-
- HY-18206A
-
-
- HY-B0231BS
-
-
- HY-107987
-
-
- HY-14325
-
|
L-745870
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-14325B
-
|
L-745870 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-131388
-
-
- HY-122203
-
|
PCS1055 dihydrochloride
|
mAChR
AChE
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
|
-
- HY-112257
-
|
S-23
|
Androgen Receptor
|
Metabolic Disease
|
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
|
-
- HY-P1397
-
|
RVD-Hpα
|
Cannabinoid Receptor
|
|
|
RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
-
- HY-B0282
-
-
- HY-101281A
-
|
(Rac)-VU 6008667
|
mAChR
|
Neurological Disease
|
|
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
|
-
- HY-B2158
-
-
- 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-114161
-
-
- HY-108057A
-
|
Facinicline hydrochloride
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
|
-
- HY-B0649
-
-
- HY-131004
-
|
CB2R PAM
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.
|
-
- HY-135572
-
-
- HY-42849
-
-
- HY-42849A
-
-
- HY-112912
-
|
P-gp modulator 1
|
P-glycoprotein
|
Cancer
|
|
P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
|
-
- HY-109592
-
-
- HY-B0231AS
-
-
- HY-114161A
-
-
- HY-N2165
-
-
- HY-N4090
-
-
- HY-B0723S
-
|
Ospemifene D4
FC-1271a D4
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
|
-
- HY-14418
-
|
VU0361737
ML-128
|
mGluR
|
Neurological Disease
|
|
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
|
-
- HY-N9326
-
|
Uralenol
|
Phosphatase
|
Metabolic Disease
|
|
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies.
|
-
- HY-P2141
-
|
TRV-120027
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
|
-
- HY-P2141A
-
|
TRV-120027 TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
|
-
- HY-17497S
-
-
- HY-11052A
-
|
Trap-101 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
|
-
- HY-B0005A
-
|
Toremifene
Z-Toremifene; NK 622 free base; FC-1157a free base
|
Estrogen Receptor/ERR
|
Cancer
Infection
|
|
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-101106
-
|
AR7
|
RAR/RXR
|
Cancer
Neurological Disease
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- HY-12237
-
-
- HY-10847A
-
|
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-100406
-
|
(S)-MCPG
(+)-MCPG
|
mGluR
|
Neurological Disease
|
|
(S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning.
|
-
- HY-126941
-
|
Hecogenin acetate
|
Opioid Receptor
|
Neurological Disease
|
|
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
|
-
- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
-
- HY-115613
-
|
ML-180
SR1848
|
Others
|
Cancer
|
|
ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.
|
-
- HY-14551
-
-
- HY-133189
-
-
- HY-100290
-
-
- HY-107734
-
-
- HY-121149
-
|
Droloxifene
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-108714
-
-
- 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-130842
-
-
- HY-P1302
-
|
Orphanin FQ(1-11)
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.
|
-
- 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-123854
-
-
- HY-B1478
-
-
- HY-19758A
-
|
Sirtuin modulator 1
|
Sirtuin
|
Cancer
|
|
Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
|
-
- HY-121392
-
-
- HY-P1216
-
|
HS014
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
|
-
- HY-103118
-
|
PU02
|
5-HT Receptor
Apoptosis
|
Cancer
Neurological Disease
|
|
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
|
-
- HY-90010
-
|
Tolterodine tartrate
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
|
|
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-P1302A
-
|
Orphanin FQ(1-11) TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.
|
-
- HY-103187
-
-
- HY-16969
-
|
Dihexa
PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2
|
c-Met/HGFR
|
Neurological Disease
|
|
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease.
|
-
- HY-112819
-
-
- HY-16579
-
|
Etifoxine hydrochloride
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-B0005
-
|
Toremifene citrate
Z-Toremifene citrate; NK 622; FC-1157a
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Infection
|
|
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-16579A
-
|
Etifoxine
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-W001909
-
|
Myosmine
|
nAChR
|
Metabolic Disease
|
|
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.
|
-
- HY-133533
-
-
- HY-70002B
-
-
- HY-N0411
-
|
β-Carotene
Provitamin A; beta-Carotene
|
Endogenous Metabolite
ROS
Apoptosis
|
Cancer
Metabolic Disease
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
|
-
- HY-103200
-
-
- HY-100672
-
-
- HY-118743
-
|
KMN-80
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
|
-
- HY-130800
-
|
Cereblon modulator 1
|
Ligand for E3 Ligase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).
|
-
- HY-128831
-
-
- HY-114314
-
|
BA-53038B
|
HBV
|
Infection
|
|
BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
|
-
- HY-15469
-
-
- 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-133014
-
-
- HY-128584
-
|
VU6005806
AZN-00016130
|
mAChR
|
Neurological Disease
|
|
VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
|
-
- HY-116463D
-
|
(Rac)-E1R
|
Sigma Receptor
|
Neurological Disease
|
|
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
|
-
- HY-10936
-
|
S 18986
|
iGluR
|
Neurological Disease
|
|
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
|
-
- HY-125112
-
-
- HY-P1216A
-
|
HS014 TFA
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
|
-
- HY-13418A
-
|
Dorsomorphin
Compound C; BML-275
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
|
-
- HY-103090
-
-
- HY-103090A
-
-
- HY-19487
-
-
- HY-101858
-
-
- 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-15470
-
-
- 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-P2497
-
-
- HY-133113
-
-
- HY-P1345
-
|
TLQP-21
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- 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-114739
-
|
MA-0204
|
PPAR
|
Metabolic Disease
|
|
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
|
-
- HY-103568
-
|
YM-298198 hydrochloride
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
|
-
- HY-16563
-
|
Narciclasine
Lycoricidinol
|
ROCK
|
Cancer
|
|
Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
|
-
- HY-136651
-
|
BNTA
|
Others
|
Inflammation/Immunology
|
|
BNTA, a potent extracellular matrix (ECM) modulator, facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA shows a promising potential for osteoarthritis alleviation by modulating cartilage generation.
|
-
- HY-108677
-
|
L-368,899 hydrochloride
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.
|
-
- 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-P1313A
-
-
- HY-P1345A
-
|
TLQP-21 TFA
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-111386
-
-
- HY-N0273
-
|
Brassinolide
Brassin lactone
|
Apoptosis
|
Cancer
|
|
Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
|
-
- HY-18705
-
-
- HY-128829
-
-
- HY-114424A
-
-
- HY-114424
-
-
- HY-P1236
-
-
- HY-N2021A
-
-
- 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-134494
-
|
MS48107
|
Others
|
Neurological Disease
|
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
|
-
- HY-123489
-
-
- HY-10121
-
-
- HY-12206
-
|
Thioperamide
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
|
-
- HY-111269
-
-
- HY-16716
-
-
- HY-101488
-
-
- HY-B1405
-
-
- HY-112788
-
-
- HY-100550
-
|
MSDC 0160
Mitoglitazone; CAY10415
|
Insulin Receptor
Mitochondrial Metabolism
|
Neurological Disease
Endocrinology
|
|
MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
|
-
- HY-B0592S
-
-
- HY-P1236A
-
-
- HY-13418
-
|
Dorsomorphin dihydrochloride
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
|
-
- HY-13728
-
|
Plevitrexed
ZD 9331; BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
|
-
- HY-130680
-
|
Syk-IN-3
|
Syk
|
Cancer
|
|
Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
|
-
- HY-136621
-
-
- HY-100507
-
|
Avadomide
CC 122
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
|
-
- HY-135581
-
|
Raloxifene 6-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-12355
-
|
Siponimod
BAF-312
|
LPL Receptor
|
Others
|
|
Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis.
|
-
- HY-135582
-
|
Raloxifene 4'-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-N7272
-
|
Cirsimarin
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase.
|
-
- HY-135147
-
|
ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-112564
-
-
- HY-117291A
-
-
- HY-15476
-
-
- HY-12158
-
|
VU0238441
|
mAChR
|
Neurological Disease
|
|
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.
|
-
- HY-14249
-
-
- HY-101093
-
-
- 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-P1471
-
-
- HY-107661
-
|
Arundic Acid
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
|
-
- HY-12812
-
|
Autotaxin modulator 1
|
Phosphodiesterase (PDE)
|
Cancer
Neurological Disease
|
|
Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.
|
-
- HY-122445
-
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- 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-19559
-
-
- HY-107651
-
-
- HY-114775
-
-
- HY-133045
-
|
VHL Ligand 8
|
Ligand for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-131019
-
|
JF-NP-26
|
mGluR
|
Neurological Disease
|
|
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
|
-
- HY-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-B0160
-
-
- HY-12700
-
|
RO5256390
|
Others
|
Neurological Disease
|
|
RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines.
RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system.
RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
|
-
- HY-111615
-
|
J-2156
|
Somatostatin Receptor
|
Neurological Disease
|
|
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
|
-
- HY-13058B
-
-
- HY-101291
-
-
- HY-13262
-
-
- HY-U00282
-
-
- HY-Y0248A
-
-
- HY-16940
-
|
24(S)-Hydroxycholesterol
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
|
-
- HY-103112A
-
|
SB 243213 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-103112B
-
|
SB 243213
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-103112
-
|
SB 243213 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-13106
-
|
Olodanrigan
EMA401; PD-126055
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
|
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
|
-
- HY-B0661
-
-
- HY-129995
-
|
TSHR antagonist S37b
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
|
-
- HY-P1112
-
-
- HY-19720
-
|
Emixustat
ACU-4429
|
Others
|
Metabolic Disease
|
|
Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
|
-
- 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-W015332
-
|
Captopril EP Impurity D
3-Bromoisobutyric acid
|
Others
|
Others
|
|
Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-137768
-
|
Captopril EP Impurity B
|
Others
|
Others
|
|
Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-W013886
-
|
Captopril EP Impurity J
S-Acetylcaptopril
|
Others
|
Others
|
|
Captopril EP Impurity J is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-137769
-
|
Captopril EP Impurity C
3-Mercaptoisobutyric acid
|
Others
|
Others
|
|
Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-B0592
-
|
Trandolapril
RU44570
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (RU44570) is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
|
-
- HY-137772
-
|
Captopril EP Impurity E
|
Others
|
Others
|
|
Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-128830
-
|
Kv3 modulator 3
|
Potassium Channel
|
Inflammation/Immunology
|
|
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
|
-
- 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-133552
-
|
RORγt Inverse agonist 10
|
ROR
|
Inflammation/Immunology
|
|
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
|
-
- HY-136208
-
|
TAN-452
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
|
-
- HY-111615A
-
|
J-2156 TFA
|
Somatostatin Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
|
-
- HY-14407
-
-
- HY-P1471A
-
|
Adrenomedullin (AM) (22-52), human TFA
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
|
-
- HY-101855
-
|
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
|
-
- HY-P1112A
-
-
- 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-14407A
-
-
- HY-113044
-
-
- HY-116144
-
|
Picaridin
Lcaridin
|
Parasite
|
Infection
|
|
Picaridin (Lcaridin) is a broad spectrum arthropod repellent. The repellent and deterrent activities of Picaridin involve olfactory sensing in mosquitoes, and ticks, via their interactions with odorant receptor proteins.
|
-
- HY-W063968
-
|
RO8191
CDM-3008; RO4948191
|
IFNAR
JAK
STAT
HCV
HBV
|
Infection
|
|
RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
|
-
- HY-B1803A
-
|
Tracazolate hydrochloride
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
|
-
- HY-16766
-
-
- HY-18292
-
-
- HY-100728
-
-
- HY-100298
-
-
- HY-111498
-
-
- HY-116463B
-
-
- HY-116463A
-
-
- HY-116463C
-
-
- HY-19608
-
-
- 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-14648
-
-
- HY-109112
-
|
Brilaroxazine
RP5063
|
Dopamine Receptor
5-HT Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
|
-
- HY-B1390B
-
-
- HY-111536
-
-
- HY-17590
-
-
- HY-125880
-
-
- HY-112282
-
-
- HY-Y0272
-
-
- HY-114372
-
|
Lycopodine
|
Lipoxygenase
Caspase
Apoptosis
|
Cancer
|
|
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
|
-
- HY-12005
-
|
Fingolimod hydrochloride
FTY720
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
|
Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
|
-
- 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-108495
-
|
CYM50308
ML248
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
|
-
- HY-108847
-
|
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-100234A
-
-
- HY-100234
-
-
- HY-112633
-
-
- HY-15446
-
|
Basimglurant
RG7090; CTEP Derivative
|
mGluR
|
Neurological Disease
|
|
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
|
-
- HY-107456
-
-
- HY-13574A
-
|
Biricodar
VX-710
|
P-glycoprotein
|
Cancer
|
|
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
|
-
- HY-17606
-
|
Cenerimod
ACT-334441
|
LPL Receptor
|
Inflammation/Immunology
|
|
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
|
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- 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-12598
-
|
(S)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
(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.
|
-
- 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-135882
-
-
- HY-107508
-
|
VU-29
|
mGluR
|
Neurological Disease
|
|
VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
|
-
- HY-107380A
-
|
PGlu-3-methyl-His-Pro-NH2 TFA
A-42872 TFA
|
Others
|
Endocrinology
|
|
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-133044
-
|
Boc-Pip-alkyne-Ph-COOH
|
PROTAC Linker
|
Cancer
|
|
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-100084
-
-
- HY-15204
-
-
- HY-109037
-
|
Mavacamten
MYK461; SAR439152
|
Myosin
|
Cardiovascular Disease
|
|
Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
-
- HY-P1562
-
|
PUMA BH3
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-U00013
-
|
Nitroflurbiprofen
HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen
|
COX
|
Cardiovascular Disease
|
|
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
|
-
- HY-112920
-
|
TM-25659
|
Others
|
Metabolic Disease
|
|
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
|
-
- HY-19589
-
-
- HY-110237
-
|
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-124958
-
|
NDMC101
|
NF-κB
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
|
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
|
-
- HY-B1221
-
|
Flufenamic acid
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-N6932
-
-
- HY-15319
-
-
- HY-135881
-
|
OMDM-5
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
|
-
- HY-N7450
-
-
- 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-76569
-
|
Desfesoterodine
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
|
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
|
-
- HY-106244A
-
|
DOTATATE acetate
|
Others
|
Cancer
|
|
DOTATATE acetate is a DOTA-conjugated peptide. DOTATATE acetate can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).
|
-
- HY-A0030
-
|
Fesoterodine fumarate
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).
|
-
- HY-70053
-
|
Fesoterodine
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB).
|
-
- HY-111098
-
-
- HY-10043
-
-
- HY-137204
-
-
- HY-119810
-
|
Seletracetam
Ucb 44212
|
Others
|
Neurological Disease
|
|
Seletracetam (Ucb 44212) is an analog of the antiepileptic agent Levetiracetam. Seletracetam is a small molecule SV2A modulator for the research of epilepsy.
|
-
- HY-114381
-
-
- 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-124733A
-
-
- HY-12640
-
|
Pyrantel pamoate
Pyrantel embonate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel pamoate (Pyrantel embonate), a tetrahydropyrimidine broad-spectrum anthelmintic, 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-133073
-
|
CCR7 Ligand 1
CCR7-Cmp2105
|
CCR
Ligand for Target Protein for PROTAC
|
Cancer
|
|
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
|
-
- HY-15319A
-
|
(±)-AMG 487
|
CXCR
|
Cancer
|
|
(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
|
-
- HY-135303
-
|
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-114269
-
-
- HY-103035
-
-
- HY-131658
-
|
VEGFR-2-IN-6
|
VEGFR
|
Others
|
|
VEGFR-2-IN-6 (example 64) is a VEGFR2 inhibitor (angiogenesis modulator), which is extracted from patent WO 02/059110.
|
-
- HY-U00151
-
-
- HY-70053A
-
|
Fesoterodine L-mandelate
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).
|
-
- HY-100634
-
|
4-Hydroxypropranolol hydrochloride
(±)-4-hydroxy Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-16489A
-
|
Terodiline hydrochloride
|
mAChR
Calcium Channel
|
Neurological Disease
|
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.
|
-
- HY-B0195
-
-
- HY-N2298
-
|
Camellianin A
|
Apoptosis
|
Cancer
|
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-B0195A
-
-
- 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-111751
-
|
JNJ-61432059
|
iGluR
|
Neurological Disease
|
|
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.
|
-
- HY-110143
-
|
CLP257
|
Potassium Channel
|
Neurological Disease
|
|
CLP257 is a selective K +-Cl − cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl − transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
|
-
- HY-13456
-
|
LY-404187
|
iGluR
|
Neurological Disease
|
|
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
|
-
- HY-136561
-
|
GRK5-IN-2
|
Others
|
Metabolic Disease
|
|
GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
|
-
- HY-124733
-
-
- HY-112055
-
|
DIM-C-pPhOH
|
Apoptosis
|
Cancer
|
|
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
|
-
- HY-W014102
-
-
- HY-12505
-
|
CX546
|
iGluR
Autophagy
|
Neurological Disease
|
|
CX546 is a first-generation and selective benzamide-type positive AMPAR modulator. CX546 is a prototypical ampakine agent and has antipsychotic effects.
|
-
- HY-107661A
-
|
S-(+)-Arundic Acid
(S)ONO-2506; (S)-2-Propyloctanoic acid
|
Others
|
Others
|
|
S-(+)-Arundic Acid ((S)ONO-2506) is the S-enantiomer of Arundic Acid. Arundic acid is an astrocyte-modulating agent, has the potential for stroke and Alzheimer’s disease research.
|
-
- HY-N2487
-
-
- HY-U00068
-
-
- HY-W010452
-
-
- HY-10043A
-
-
- HY-N2370
-
-
- HY-113378
-
-
- HY-108625
-
|
SHA 68
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
|
-
- HY-B0589C
-
|
(3S,5S)-Atorvastatin
|
Cytochrome P450
|
Metabolic Disease
|
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-12452
-
-
- HY-108511A
-
|
PB28
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Cancer
Infection
|
|
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
|
-
- 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-13965
-
|
Parmodulin 2
ML161
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
|
-
- HY-100371
-
|
(RS)-MCPG
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-14425
-
-
- HY-N2032
-
|
Euphorbiasteroid
|
AMPK
|
Cancer
Infection
Metabolic Disease
|
|
Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
|
-
- HY-120722
-
|
TCH-165
|
Proteasome
|
Cancer
|
|
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
|
-
- HY-18007
-
-
- HY-14399
-
-
- HY-12212
-
-
- HY-14316A
-
|
Tebanicline dihydrochloride
Ebanicline dihydrochloride; ABT-594 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
|
-
- HY-121618
-
|
α-Thujone
|
GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
|
-
- HY-119437
-
|
FLTX1
|
Estrogen Receptor/ERR
|
Cancer
|
|
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
|
-
- HY-119165
-
-
- HY-129395
-
|
CC-92480
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.
|
-
- HY-N3308
-
|
Medicarpin
|
Apoptosis
|
Cancer
|
|
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs.
|
-
- HY-114406
-
|
TD-106
|
Ligand for E3 Ligase
|
Cancer
|
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
|
-
- HY-107409
-
|
GNE 5729
|
iGluR
|
Neurological Disease
|
|
GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
|
-
- HY-W010104
-
-
- HY-128400
-
|
4'-Methoxychalcone
|
PARP
|
Metabolic Disease
Cancer
|
|
4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
|
-
- HY-109187A
-
|
Posenacaftor sodium
PTI-801 sodium
|
CFTR
|
Inflammation/Immunology
|
|
Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).
|
-
- HY-100588
-
|
VU0364770
|
mGluR
|
Neurological Disease
|
|
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
|
-
- HY-100588A
-
|
VU0364770 hydrochloride
|
mGluR
|
Neurological Disease
|
|
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
|
-
- HY-133011
-
|
nAChR agonist 1
|
nAChR
|
Neurological Disease
|
|
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
|
-
- HY-16636
-
|
ML337
|
mGluR
|
Neurological Disease
|
|
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile.
|
-
- HY-131181
-
|
LEI-401
|
Phospholipase
|
Neurological Disease
|
|
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.
|
-
- HY-14886
-
-
- HY-121538
-
|
CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-120530
-
|
JNJ-46281222
|
mGluR
|
Neurological Disease
|
|
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
|
-
- HY-108337
-
|
GNE-0723
|
iGluR
|
Neurological Disease
|
|
GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
|
-
- HY-125740
-
|
Malvidin-3-glucoside chloride
Malvidin-3-O-glucoside chloride; Oenin chloride
|
Others
|
Inflammation/Immunology
|
|
Malvidin-3-glucoside chloride (Malvidin-3-O-glucoside chloride), a major wine anthocyanin, is effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation.
|
-
- HY-107902
-
-
- HY-105858
-
|
BNC210
H-Ile-Trp-OH; IW-2143
|
nAChR
|
Neurological Disease
|
|
BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
|
-
- HY-12151
-
|
NS 1738
NSC 213859
|
nAChR
|
Neurological Disease
|
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
|
-
- HY-131997
-
|
2'MeO6MF
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
|
-
- 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-100634S
-
|
4-Hydroxypropranolol D7 hydrochloride
(±)-4-hydroxy Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-N2585
-
|
Isodeoxyelephantopin
|
Reactive Oxygen Species
NF-κB
Autophagy
|
Cancer
|
|
Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
|
-
- HY-14859
-
|
Dipraglurant
ADX48621
|
mGluR
|
Neurological Disease
|
|
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.
|
-
- HY-129527
-
|
GNE-9278
|
iGluR
|
Neurological Disease
|
|
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
|
-
- HY-W011509
-
-
- HY-B0368
-
|
Captopril
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
|
-
- HY-15371
-
|
Forskolin
Coleonol; Colforsin
|
Adenylate Cyclase
FXR
Autophagy
|
Cancer
Endocrinology
Metabolic Disease
Inflammation/Immunology
|
|
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
|
-
- 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-107774
-
|
BMS-986163
|
iGluR
|
Neurological Disease
|
|
BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
|
-
- HY-12795
-
|
Vps34-IN-1
|
PI3K
Autophagy
|
Cancer
|
|
Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
|
-
- HY-101792A
-
|
RG7800 hydrochloride
RO6885247 hydrochloride
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.
|
-
- HY-103575A
-
|
MFZ 10-7 hydrochloride
|
mGluR
|
Neurological Disease
|
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
|
-
- HY-134194
-
|
KL201
|
Others
|
Metabolic Disease
|
|
KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues.
|
-
- HY-B1837
-
|
Cyfluthrin
|
Sodium Channel
|
Infection
|
|
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
|
-
- HY-13963
-
|
ZCL278
|
Ras
|
Cancer
|
|
ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
|
-
- HY-113962
-
|
7α,25-Dihydroxycholesterol
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
-
- HY-N2533
-
-
- HY-12404
-
|
Diminazene aceturate
Diminazene diaceturate
|
Parasite
Angiotensin-converting Enzyme (ACE)
|
Infection
Inflammation/Immunology
|
|
Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.
|
-
- HY-135795
-
|
1-Cyclohexyl-3-dodecyl urea
CDU; N-Cyclohexyl-N-dodecyl urea; NCND
|
Epoxide Hydrolase
|
Metabolic Disease
Cardiovascular Disease
|
|
1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.
|
-
- HY-119332
-
|
3-Keto petromyzonol
|
Others
|
Endocrinology
|
|
3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey.
|
-
- HY-107091
-
|
Aspartyl-alanyl-diketopiperazine
DA-DKP
|
Others
|
Inflammation/Immunology
|
|
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
|
-
- HY-14417
-
|
VU0155041
|
mGluR
|
Neurological Disease
|
|
VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
|
-
- HY-101281
-
|
VU 6008667
|
mAChR
|
Neurological Disease
|
|
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
|
-
- HY-107198
-
-
- HY-14417B
-
|
VU0155041 sodium
|
mGluR
|
Neurological Disease
|
|
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
|
-
- HY-111772
-
|
Elexacaftor
VX-445
|
CFTR
Autophagy
|
Others
|
|
Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
|
-
- HY-13058
-
|
ADX-47273
|
mGluR
|
Neurological Disease
|
|
ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
|
-
- HY-N4180
-
|
Pennogenin 3-O-beta-chacotrioside
|
Autophagy
|
Cancer
|
|
Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
|
-
- 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-136151
-
|
UNC10217938A
|
Others
|
Others
|
|
UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
|
-
- HY-116819
-
|
VU0453379
|
Glucagon Receptor
|
Metabolic Disease
|
|
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
|
-
- HY-113066
-
-
- HY-114395
-
|
NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-N0179
-
|
Ecdysone
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
|
-
- HY-113066A
-
-
- HY-128677
-
|
NCC007
|
Casein Kinase
|
Neurological Disease
|
|
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
|
-
- 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-N0029
-
|
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-N0513
-
|
Loganic acid
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
|
-
- HY-N6694
-
-
- HY-111828
-
|
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-15015
-
-
- HY-15015A
-
-
- HY-P1222
-
|
LL-37, human
|
Bacterial
|
Infection
|
|
LL-37, human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, human could help protect the cornea from infection and modulates wound healing.
|
-
- HY-122487
-
|
Troriluzole
BHV-4157
|
Others
|
Neurological Disease
|
|
Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
|
-
- HY-115467
-
|
MitoBloCK-10
|
Others
|
Metabolic Disease
|
|
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
|
-
- HY-114933
-
|
VU0119498
|
mAChR
|
Metabolic Disease
|
|
VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity.
|
-
- HY-123956
-
|
HG-12-6
|
IRAK
|
Inflammation/Immunology
|
|
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
|
-
- HY-15477A
-
|
YS-49 monohydrate
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-15477
-
|
YS-49
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-17537
-
|
APY29
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
|
-
- HY-128776
-
|
Antitumor agent-19
|
Others
|
Cancer
|
|
Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
|
-
- HY-B0719
-
|
Ingenol Mebutate
Ingenol 3-angelate; PEP005
|
PKC
|
Cancer
Inflammation/Immunology
|
|
Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
|
-
- HY-N2360
-
|
Hinokiflavone
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
|
-
- HY-126145
-
-
- HY-111475
-
-
- HY-P1222A
-
|
LL-37, human TFA
|
Bacterial
|
Infection
|
|
LL-37, human TFA is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, human TFA could help protect the cornea from infection and modulates wound healing.
|
-
- 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-P3102
-
|
GLP-1(32-36)amide
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.
|
-
- HY-N0781
-
|
Linderalactone
|
Apoptosis
|
Cancer
|
|
Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
|
-
- HY-15656S
-
-
- HY-124759
-
-
- 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-108258A
-
|
PSN 375963 hydrochloride
|
GPR119
|
Endocrinology
|
|
PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
|
-
- HY-14364
-
-
- 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-P1303
-
|
CART(62-76)(human,rat)
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-100933
-
-
- 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-B1805
-
|
Triclocarban
3,4,4′-Trichlorocarbanilide
|
Bacterial
|
Infection
|
|
Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes.
|
-
- HY-129811
-
|
Bis-ANS dipotassium
|
Microtubule/Tubulin
|
Neurological Disease
|
|
Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations.
|
-
- HY-124614
-
|
GLP-26
|
HBV
|
Infection
|
|
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.
GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
|
-
- HY-N6950
-
|
Hederacolchiside A1
|
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Cancer
Infection
|
|
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
|
-
- HY-122579
-
|
IGS-1.76
|
Others
|
Others
|
|
IGS-1.76 efficiently inhibits the human NCS-1/Ric8a complex. IGS-1.76 shows a significantly increased affinity for hNCS-1 and is able to modulate the hNCS-1/Ric8a interaction efficiently.
|
-
- HY-P3102A
-
-
- HY-135909
-
|
TH1217
ZINC1775962367
|
SARS-CoV
|
Cancer
Infection
|
|
TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
|
-
- HY-P1303A
-
|
CART(62-76)(human,rat) TFA
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-122590
-
|
Glabrescione B
|
Gli
|
Cancer
|
|
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
|
-
- HY-17614
-
|
Ezutromid
SMT C1100; BMN 195; VOX-C1100
|
Others
|
Others
|
|
Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
|
-
- HY-122559
-
|
BMS-984923
|
mGluR
|
Neurological Disease
|
|
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
|
-
- HY-120789
-
|
PF-06648671
|
γ-secretase
|
Neurological Disease
|
|
PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
|
-
- HY-104037
-
|
Cintirorgon
LYC-55716
|
ROR
|
Cancer
|
|
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.
|
-
- HY-N0313
-
|
Euphol
|
Endogenous Metabolite
MAGL
|
Inflammation/Immunology
|
|
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
|
-
- HY-136866
-
|
Aβ42-IN-2
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of Alzheimer's disease.
|
-
- HY-115579
-
|
MALAT1-IN-1
|
Others
|
Cancer
|
|
MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
|
-
- HY-12949
-
|
ML204
|
TRP Channel
|
Neurological Disease
|
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-12949A
-
|
ML204 hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-N0067
-
-
- HY-119695A
-
|
Simvastatin acid ammonium
Tenivastatin ammonium
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
|
-
- HY-117639
-
|
AUT1
|
Potassium Channel
|
Cancer
|
|
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
|
-
- HY-N6843
-
|
Arnicolide D
|
Caspase
PI3K
Akt
mTOR
STAT
|
Cancer
|
|
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
|
-
- HY-P2076A
-
|
Dusquetide TFA
SGX942 TFA
|
Bacterial
|
Cancer
Infection
|
|
Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
-
- HY-114395A
-
|
(R)-NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
(R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-N7695
-
|
Physalin B
|
Apoptosis
Autophagy
|
Cancer
|
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro.
|
-
- 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-14393
-
|
Emodin
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
|
Cancer
|
|
Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
|
-
- HY-U00251
-
-
- HY-116564
-
|
Lotilaner
|
Parasite
GABA Receptor
|
Infection
|
|
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-106225
-
|
Rotigaptide
ZP123
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
|
-
- HY-W011733
-
-
- HY-109139
-
-
- HY-P0201
-
-
- HY-P1209A
-
-
- HY-50175
-
-
- HY-P1209
-
-
- HY-A0007
-
-
- HY-10016
-
|
E 2012
|
γ-secretase
|
Neurological Disease
|
|
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
|
-
- HY-14600
-
-
- HY-B2163
-
|
Astaxanthin
|
PPAR
Reactive Oxygen Species
|
Cancer
Cardiovascular Disease
|
|
Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
|
-
- HY-121508
-
|
(E/Z)-IT-603
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
|
-
- HY-12152
-
|
PNU-120596
NSC 216666
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
|
-
- HY-102070
-
|
NS13001
|
Potassium Channel
|
Neurological Disease
|
|
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
|
-
- HY-15539
-
-
- HY-P0216
-
-
- HY-15394
-
-
- HY-B0895
-
-
- HY-P1481
-
-
- HY-B0461
-
|
Trospium chloride
|
mAChR
|
Neurological Disease
|
|
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors.
|
-
- HY-P0201A
-
-
- HY-13274
-
-
- HY-124634
-
|
PZ-2891
|
Others
|
Neurological Disease
|
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
|
-
- HY-10794
-
-
- HY-P1030
-
-
- 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-P2307
-
|
Tat-NR2Baa
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-P2307A
-
|
Tat-NR2Baa TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-18347A
-
-
- HY-14218
-
-
- HY-101038A
-
-
- HY-19250
-
-
- HY-76612
-
-
- HY-14127
-
|
R121919
NBI30775
|
CRFR
|
Neurological Disease
Endocrinology
|
|
R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
|
-
- HY-103104
-
|
Fananserin
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
|
-
- HY-107723
-
-
- HY-15498
-
|
Rimegepant
BMS-927711
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
|
-
- HY-P2546
-
|
Biotin-Substance P
|
Neurokinin Receptor
|
Neurological Disease
|
|
Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
|
-
- HY-B1640
-
|
Ethacrynic acid
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-128895
-
|
KL1333
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures.
|
-
- HY-N2499
-
|
Dehydrotumulosic acid
|
Others
|
Metabolic Disease
|
|
Dehydrotumulosic acid, one of the effective constituents of Poria cocos, was isolated from the chloroform-soluble material of ethanol extract of the fungus. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body.
|
-
- HY-12749
-
-
- HY-13101
-
-
- HY-103533
-
-
- 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-14335
-
|
Ro 04-6790
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors.
|
-
- HY-120874
-
|
PF-06372865
|
GABA Receptor
|
Neurological Disease
|
|
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
|
-
- HY-10418
-
-
- HY-B1270
-
-
- HY-101626
-
-
- HY-15039
-
|
SSR240612
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-112558
-
-
- HY-12749A
-
-
- HY-U00253
-
-
- HY-B0412
-
-
- HY-B0469
-
-
- 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-101641
-
-
- 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-16751
-
-
- 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-136587
-
|
Oxomemazine
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment.
|
-
- HY-128686
-
|
KAG-308
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.
|
-
- HY-N6727
-
|
Gliotoxin
Aspergillin
|
Apoptosis
PKA
NF-κB
Bacterial
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
|
-
- HY-N6022
-
|
Byakangelicin
|
Others
|
Metabolic Disease
|
|
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
|
-
- HY-P1075
-
|
CALP3
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- HY-19620
-
|
Branaplam
LMI070; NVS-SM1
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
|
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
|
-
- HY-15195
-
-
- HY-14870
-
-
- HY-10634
-
-
- HY-136209
-
|
SU5208
|
VEGFR
|
Cancer
|
|
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2).
|
-
- HY-19308
-
-
- HY-15541
-
-
- HY-17551
-
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-101957
-
|
AG 1295
|
PDGFR
|
Cardiovascular Disease
|
|
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
|
-
- HY-W010841
-
|
Levocetirizine dihydrochloride
(R)-Cetirizine dihydrochloride
|
Histamine Receptor
|
Endocrinology
Inflammation/Immunology
|
|
Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
|
-
- HY-B0814
-
|
Levocetirizine
(R)-Cetirizine
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
|
-
- HY-124283A
-
|
LEI-101
|
Cannabinoid Receptor
|
Neurological Disease
|
|
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
|
-
- HY-P1423A
-
|
BA 1 TFA
|
Bombesin Receptor
|
Cancer
Metabolic Disease
|
|
BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
|
-
- HY-P1423
-
|
BA 1
|
Bombesin Receptor
|
Cancer
Metabolic Disease
|
|
BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
|
-
- HY-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-111767
-
|
BAY-545
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
|
-
- HY-118557
-
|
Iferanserin
S-MPEC
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment.
|
-
- HY-B1281
-
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- 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-50675
-
-
- HY-16756
-
-
- HY-B0726
-
-
- HY-10486
-
-
- HY-105018
-
|
Epelsiban
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-112720
-
-
- HY-19733
-
-
- HY-108912
-
-
- HY-100714A
-
|
D-AP5
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
|
-
- HY-W011955
-
-
- HY-101653
-
|
MHP 133
|
AChE
mAChR
5-HT Receptor
|
Neurological Disease
|
|
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
|
-
- HY-14743B
-
|
Golotimod hydrochloride
SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
|
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-108538
-
|
Ethacrynic acid D5
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-113466
-
|
4-Hydroxynonenal
4-HNE
|
Aldehyde Dehydrogenase (ALDH)
Endogenous Metabolite
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
-
- HY-107390A
-
|
AX-024 hydrochloride
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-15672
-
|
FM19G11
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Neurological Disease
|
|
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
|
-
- HY-10514
-
|
BX795
|
PDK-1
IKK
Autophagy
|
Cancer
|
|
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
|
-
- HY-136190
-
|
TRPC6-PAM-C20
|
TRP Channel
|
|
|
TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
|
-
- HY-P0063
-
|
Copper tripeptide
GHK-Cu
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
|
-
- HY-100403
-
|
Ro 67-7476
|
mGluR
|
Cancer
|
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
|
-
- HY-N2557
-
|
Euphorbia Factor L1
|
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect.
|
-
- HY-135276
-
|
Targaprimir-96
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
|
-
- HY-103484
-
|
GATA4-NKX2-5-IN-1
|
Others
|
Cardiovascular Disease
|
|
GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
|
-
- HY-107390
-
|
AX-024
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-17615
-
-
- HY-B1006
-
-
- HY-101420
-
-
- HY-P1467
-
-
- HY-118180
-
-
- HY-U00077
-
-
- HY-19048
-
-
- HY-113356
-
-
- HY-B0548S1
-
-
- HY-70068
-
-
- HY-109095
-
-
- HY-15445
-
|
CTEP
RO 4956371; mGluR5 inhibitor
|
mGluR
|
Neurological Disease
|
|
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
|
-
- HY-B1794A
-
-
- HY-135892
-
|
GNE-1858
|
MAP4K
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
|
-
- HY-117508
-
-
- HY-B1693
-
|
Levomepromazine
Methotrimeprazine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Levomepromazine (Methotrimeprazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors.
|
-
- HY-100301
-
-
- 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-125839
-
-
- HY-P2510
-
-
- HY-P1467A
-
-
- HY-15538
-
-
- HY-U00302
-
-
- HY-12940
-
-
- HY-P1588
-
-
- HY-121877
-
|
Valnoctamide
Valmethamide
|
GABA Receptor
|
Neurological Disease
|
|
Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors.
|
-
- HY-10900
-
-
- HY-13788
-
-
- HY-Y1683
-
|
DL-Menthol
Racementhol
|
GABA Receptor
|
Others
|
|
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol induces surgical anesthesia for fish that relates to the activation of GABAA receptor.
|
-
- HY-100856
-
-
- HY-101333
-
|
CPPG
(RS)-CPPG
|
mGluR
|
Neurological Disease
|
|
CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
|
-
- HY-A0077
-
|
Perphenazine
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- 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-11030
-
-
- 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-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-112603
-
|
AP5
|
GPR40
|
Metabolic Disease
|
|
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
|
-
- HY-19365
-
-
- HY-17428
-
-
- HY-128975
-
-
- HY-15540
-
-
- HY-15653
-
-
- HY-13338S
-
-
- HY-N0835
-
-
- HY-12127
-
-
- HY-17351
-
-
- HY-P1107
-
|
Antisauvagine-30
aSvg-30
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively.
|
-
- HY-16963
-
-
- HY-110000
-
-
- 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-107563A
-
|
ROS 234 dioxalate
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
|
-
- HY-B0623A
-
|
Ropinirole hydrochloride
SKF 101468 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
|
-
- HY-103286
-
|
PD176252
|
Bombesin Receptor
|
Cancer
|
|
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
|
-
- HY-11018
-
-
- HY-B0072
-
-
- HY-P0298
-
-
- HY-P9903
-
|
Nivolumab
BMS-936558; ONO-4538; MDX-1106
|
PD-1/PD-L1
|
Cancer
|
|
Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody to treat advanced (metastatic) non-small cell lung cancer.
|
-
- HY-P0298A
-
-
- HY-15370
-
-
- HY-B0469S
-
-
- HY-N1166
-
|
Tephrosin
Deguelinol I; Hydroxydeguelin
|
EGFR
|
Cancer
|
|
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
|
-
- HY-U00341
-
-
- HY-10021
-
-
- HY-B0377
-
-
- HY-U00238
-
-
- HY-111372
-
|
Finerenone
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
|
-
- HY-103295A
-
-
- HY-10797
-
|
CJ-42794
CJ-042794
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
CJ-42794 is a selective prostaglandin E receptor subtype 4
(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
|
-
- HY-14873
-
|
Tonapofylline
BG 9928
|
Adenosine Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
|
-
- HY-119163
-
-
- 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-N2003
-
|
D-Tetrahydropalmatine
|
Dopamine Receptor
|
Metabolic Disease
|
|
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
|
-
- HY-P1218
-
|
Phrixotoxin 3
|
Sodium Channel
|
Neurological Disease
|
|
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
|
-
- HY-120355A
-
|
AP14145 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
|
-
- HY-105231
-
|
Bryostatin 1
|
PKC
HIV
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
|
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
|
-
- HY-14743
-
|
Golotimod
SCV 07; Gamma-D-glutamyl-L-tryptophan
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
|
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-117482
-
|
BPN-15606
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
|
-
- HY-130609A
-
|
Aβ42-IN-1 free base
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
|
-
- HY-N1427A
-
-
- HY-100248
-
-
- HY-100810
-
-
- HY-B0031S
-
-
- HY-13044
-
-
- HY-13604
-
-
- HY-U00185
-
-
- HY-B0732
-
-
- HY-112840
-
-
- HY-P1462
-
-
- HY-14825
-
|
Tarafenacin
SVT-40776
|
mAChR
|
Neurological Disease
|
|
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-101619
-
-
- HY-P1481A
-
-
- HY-10633
-
-
- HY-11018A
-
-
- HY-14277A
-
-
- HY-129029
-
|
Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-11030A
-
-
- HY-13221
-
-
- HY-101980
-
|
AZD4635
HTL1071
|
Adenosine Receptor
|
Cancer
|
|
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
|
-
- HY-10171
-
|
NPS-2143 hydrochloride
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-10007
-
|
NPS-2143
SB-262470A
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-103110A
-
|
ST1936 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.
|
-
- HY-A0168
-
|
Regadenoson
CVT-3146
|
Adenosine Receptor
|
Cardiovascular Disease
Cancer
|
|
Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents.
|
-
- HY-14544
-
|
Quetiapine
ICI204636
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
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- HY-B0031
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Quetiapine hemifumarate
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
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- HY-15419
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RS-127445 hydrochloride
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5-HT Receptor
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Neurological Disease
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RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
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- HY-B0436
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- HY-19533
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SCH 58261
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Adenosine Receptor
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Cancer
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SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
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- HY-14567
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Ciproxifan
FUB-359
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Histamine Receptor
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Neurological Disease
Endocrinology
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Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease.
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- HY-B0781
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- HY-15419A
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RS-127445
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5-HT Receptor
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Neurological Disease
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RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
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- HY-15289
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Ciproxifan maleate
FUB 359 maleate
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Histamine Receptor
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Neurological Disease
Endocrinology
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Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
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- HY-15122
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- HY-13505
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- HY-I0230
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- HY-12870A
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AZD9496 maleate
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Estrogen Receptor/ERR
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Cancer
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AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
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- HY-138558
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- HY-P1462A
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- HY-B0164A
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- HY-10889
