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Results for "

negative allosteric modulator (NAMs)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (1) Cannabinoid Receptor (2) Dopamine Receptor (1) ERK (2) Estrogen Receptor/ERR (1) GABA Receptor (4) GCGR (1) LPL Receptor (1) mAChR (3) mGluR (12) Src (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (2) Endocrinology (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (20)

Inhibitors & Agonists

Screening Libraries

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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-110180

VU0409106	mGluR	Neurological Disease
VU0409106 is a potent and selective mGlu₅ negative allosteric modulator (NAM) with an IC₅₀ of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .

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-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-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-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 K_i of 0.67 nM for rat mGluR5 . MFZ 10-7 (hydrochloride) 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-103575

MFZ 10-7	mGluR	Neurological Disease
MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a K_i of 0.67 nM for rat mGluR5 . MFZ 10-7 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-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-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-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-129274

RO4988546	mGluR	Neurological Disease
RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [ ³h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers .

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-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-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-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 .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library	190 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 190 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Allosteric Modulators (AMs) Compound Library

190 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 190 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

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