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Results for "

Negative allosteric

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adenosine Receptor (1) Adrenergic Receptor (1) Apoptosis (1) Atg4 (1) Autophagy (1) Calcium Channel (1) Cannabinoid Receptor (3) CaSR (4) CCR (1) Dopamine Receptor (1) Drug Isomer (1) ERK (4) Estrogen Receptor/ERR (2) Free Fatty Acid Receptor (1) GABA Receptor (7) GCGR (2) Glutaminase (1) Histone Methyltransferase (2) iGluR (13) Interleukin Related (2) Lipoxygenase (1) LPL Receptor (1) mAChR (5) Mas-related G-protein-coupled Receptor (MRGPR) (1) mGluR (54) Molecular Glues (1) P2X Receptor (5) PERK (1) Phosphodiesterase (PDE) (1) Potassium Channel (3) Protease Activated Receptor (PAR) (1) Reference Standards (10) Src (1) Urotensin Receptor (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (13) Cardiovascular Disease (3) Endocrinology (1) Infection (1) Inflammation/Immunology (10) Metabolic Disease (10) Neurological Disease (85)

By Targets:

5-HT Receptor (1)

Adenosine Receptor (1)

Adrenergic Receptor (1)

Apoptosis (1)

Atg4 (1)

Autophagy (1)

Calcium Channel (1)

Cannabinoid Receptor (3)

CaSR (4)

CCR (1)

Dopamine Receptor (1)

Drug Isomer (1)

ERK (4)

Estrogen Receptor/ERR (2)

Free Fatty Acid Receptor (1)

GABA Receptor (7)

GCGR (2)

Glutaminase (1)

Histone Methyltransferase (2)

iGluR (13)

Interleukin Related (2)

Lipoxygenase (1)

LPL Receptor (1)

mAChR (5)

Mas-related G-protein-coupled Receptor (MRGPR) (1)

mGluR (54)

Molecular Glues (1)

P2X Receptor (5)

PERK (1)

Phosphodiesterase (PDE) (1)

Potassium Channel (3)

Protease Activated Receptor (PAR) (1)

Reference Standards (10)

Src (1)

Urotensin Receptor (1)

Wnt (1)

β-catenin (1)

By Research Areas:

Cancer (13)

Cardiovascular Disease (3)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (10)

Metabolic Disease (10)

Neurological Disease (85)

116

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19996

AH-7614 Maximum Cited Publications 6 Publications Verification	Free Fatty Acid Receptor	Metabolic Disease
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC₅₀s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC₅₀<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist .

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-173156

UNC10013	Histone Methyltransferase	Cancer
UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research .

HY-122138

VU6010572 1 Publications Verification	mGluR	Neurological Disease
VU6010572 is a potent, selective and brain-penetrant mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

HY-124622

NNC-0640	GCGR	Metabolic Disease
NNC-0640 is an effective negative allosteric modulator (NAM) of the human glucagon receptor (GCGR), with an IC₅₀ value of 69.2 nM. NNC-0640 holds potential for research in the field of diabetes .

HY-124569

NAB-14	iGluR	Neurological Disease
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC₅₀ of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .

HY-108710

VU0650786 2 Publications Verification	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-148016

I-287	Protease Activated Receptor (PAR) ERK	Inflammation/Immunology
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gα_q and Gα_12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research .

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 . Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-103320A

Calhex 231 hydrochloride Maximum Cited Publications 6 Publications Verification	CaSR	Metabolic Disease
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC₅₀ = 0.39 μM) increases in [ ³H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca ²⁺-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .

HY-116553

FzM1	Wnt β-catenin	Cancer
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC_50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .

HY-101845

FITM 1 Publications Verification	mGluR	Cancer
FITM is a negative allosteric modulator of mGlu1 receptor with a K_i of 2.5 nM.

HY-124803

GPCR modulator-1	GCGR	Metabolic Disease
GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes .

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-12567

ML375 VU0483253	mAChR	Neurological Disease
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC₅₀s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .

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 (K_d high affinity of 1.7 nM and K_d low affinity of 14.5 nM) .

HY-19630

ML289 VU0463597	mGluR	Neurological Disease
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC₅₀=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-16766

Decoglurant RO4995819	mGluR	Neurological Disease
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .

HY-129946

Dopamine D2 receptor antagonist-1	Dopamine Receptor	Neurological Disease
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .

HY-110278

ADX71743	mGluR	Neurological Disease
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity. .

HY-145585

Onfasprodil MIJ-821	iGluR	Neurological Disease
Onfasprodil (MIJ-821) is a selective intravenous NMDA receptor NR2B subunit negative allosteric modulator (NAM). Onfasprodil inhibits the activity of NR2B-NMDA receptors. Onfasprodil has a rapid antidepressant effect. Onfasprodil can be used for the research of treatment-resistant depression (TRD) .

HY-164764

ADX61623	Estrogen Receptor/ERR	Endocrinology
ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease .

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-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-103320B

(1R,2R)-Calhex 231 hydrochloride	CaSR	Metabolic Disease
(1R,2R)-Calhex 231 hydrochloride is the isomer of Calhex 231 hydrochloride (HY-103320A), and can be used as an experimental control. Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca ²⁺-induced accumulation of [ ³H]inositol phosphate with an IC₅₀ of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment .

HY-129636

CLH304a (E)-GABAB receptor antagonist 1	GABA Receptor ERK	Neurological Disease
CLH304a (compound 14) is a specific and noncompetitive GABA_B receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC₅₀ of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA_B receptor .

HY-155088

MK-8768	mGluR	Metabolic Disease
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 **negative allosteric modulator (IC₅₀ of 9 .6nM) with excellent brain permeability**.

HY-177127

Satoprodil	iGluR	Neurological Disease
Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC₅₀ value of 123 nM for NR2B .

HY-103574

Raseglurant hydrochloride ADX-10059 hydrochloride	mGluR	Neurological Disease
Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .

HY-120375

LUF7346	Potassium Channel	Cardiovascular Disease
LUF7346 is a potent Kv11.1 (hERG) channel negative allosteric modulator, with an IC₅₀ of 35.6 ± 3.2 nM .

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability .

HY-14866

Raseglurant ADX-10059	mGluR	Neurological Disease
Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .

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-103572

MNI137	mGluR	Neurological Disease
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC₅₀s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .

HY-107509

LY2389575 hydrochloride	mGluR	Neurological Disease
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC₅₀ value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .

HY-124985

VU6010608	mGluR	Neurological Disease
VU6010608 is a blood-brain barrier-crossing mGlu7 negative allosteric modulator (IC₅₀ = 0.76 μM). VU6010608 can block long-term enhancement (LTP) of SC-CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 can be used for research on neurological diseases .

HY-15469

GW791343 dihydrochloride 1 Publications Verification	P2X Receptor	Neurological Disease
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC₅₀ of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .

HY-103118

PU02	5-HT Receptor Apoptosis	Neurological Disease Cancer
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-119282

AZD6538	mGluR	Neurological Disease
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC₅₀ values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .

HY-103561

DCB	mGluR	Neurological Disease
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .

HY-114863

PHCCC(4Me) THCCC	mGluR	Neurological Disease
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC₅₀ of 1.5 μM) negative allosteric modulator and mGluR3 (EC₅₀ of 8.9 μM) positive allosteric modulator .

HY-W565924

STX107	mGluR ERK	Neurological Disease
STX107 is a metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulator (NAM) with a pK_i of 8.32. STX107 inhibits glutamate-induced Ca ²⁺ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .

HY-103320

Calhex 231	CaSR	Metabolic Disease
Calhex 231 is a potent negative allosteric modulator that blocks (IC₅₀ = 0.39 μM) increases in [ ³H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca ²⁺-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .

HY-112788

ONO-8590580	GABA Receptor	Neurological Disease
ONO-8590580 is a GABA_A α5 negative allosteric modulator.

HY-110191

VU0469650	mGluR	Neurological Disease Cancer
VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM .

HY-100667

UBP608 1 Publications Verification	iGluR	Neurological Disease
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .

HY-124393

GRN-529	mGluR	Neurological Disease
GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .

HY-119377

UPGL00004	Glutaminase	Cancer
UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC₅₀=29 nM; K_d=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines .

HY-107774

BMS-986163	iGluR	Neurological Disease
BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (K_i=4 nM, IC₅₀=24 nM).

HY-115483

VU0477573	mGluR	Neurological Disease
VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

250 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 250 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Target	Research Area

HY-P11259

UPG-111	Urotensin Receptor	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .

Cat. No.	Product Name	Target	Research Area	Image

HY-P99171

Gevokizumab 2 Publications Verification	Interleukin Related	Inflammation/Immunology Cancer
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .

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