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Results for "

Negative allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (1) Calcium Channel (1) Cannabinoid Receptor (2) CaSR (2) CCR (1) Dopamine Receptor (1) ERK (2) Estrogen Receptor/ERR (1) GABA Receptor (5) GCGR (2) iGluR (7) Interleukin Related (1) LPL Receptor (1) mAChR (3) mGluR (36) P2X Receptor (3) Potassium Channel (2) Src (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (2) Endocrinology (1) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (53)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-119765

VU0366248	mGluR	Neurological Disease
VU0366248 is a mGlu5 negative allosteric modulator .

HY-145585

Onfasprodil MIJ-821	iGluR	Neurological Disease
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A) .

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-120527

VU0463841	mGluR	Neurological Disease
VU0463841 is a potent, selective and brain-penetrant mGlu5 negative allosteric modulator (NAM) with an IC₅₀ of 13 nM. VU0463841 is ineffective against mGlu1-4 and mGlu7-8. VU0463841 has the potential for the Cocaine addiction research .

HY-120428

VU0410425	mGluR	Neurological Disease
VU0410425 is an mGlu₁ negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu₁ with an IC₅₀ value of 140 nM. VU0410425 can be used for the research of central nervous system disorders .

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-157998

mG2N001	mGluR Src	Others
mG2N001 is a negative allosteric modulator (NAM) (IC₅₀: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope ^[11C]mG2N001 can be used in PET imaging. ^[11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .

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-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-129636A

(E/Z)-CLH304a GABAB receptor antagonist 1	GABA Receptor ERK	Neurological Disease
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABA_B receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .

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-120411

Sadopine	Calcium Channel	Others
Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels .

HY-147558

CB1R Allosteric modulator 1	Cannabinoid Receptor	Others
CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

HY-147559

CB1R Allosteric modulator 2	Cannabinoid Receptor	Others
CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

HY-124803

GPCR modulator-1	GCGR	Metabolic Disease
GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research .

HY-145370

GluN2B receptor modulator-1	iGluR	Neurological Disease
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC₅₀ value of 31 nM.

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-112788

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

HY-103573

VU 0360223	mGluR	Neurological Disease
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM .

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-16766

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

HY-119941

VU0652835	mGluR	Neurological Disease
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ of 81 nM .

HY-110191

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

HY-147657

GABAA receptor modulator-2	GABA Receptor	Neurological Disease
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .

HY-122138

VU6010572	mGluR	Neurological Disease
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

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-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-100667

UBP608	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-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-103491

PF-06462894	iGluR	Neurological Disease
PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates .

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-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-168028

mGluR2 modulator 5	mGluR	Neurological Disease
mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC₅₀ of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases .

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-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 .

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-108710

VU0650786 1 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-12629

PF470 PF-06297470	Others	Others
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.

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-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-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-120699

RO5488608	mGluR	Neurological Disease
RO5488608 is a negative allosteric metabotropic modulator of glutamate receptor 2/3. RO5488608 inhibits LY354740 (HY-18941)-induced intracellular Ca ²⁺ release and can be used for study of antidepressant .

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-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 .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

183 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 183 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-P99171

Gevokizumab	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) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-P99171

Gevokizumab	Classification of Application Fields Disease Research Fields Cancer	Interleukin Related
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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