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Results for "

Positive allosteric modulator (PAM)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (5) Amyloid-β (1) Calcium Channel (1) Cannabinoid Receptor (3) CaSR (4) Cholinesterase (ChE) (2) COX (6) Cytochrome P450 (3) Dopamine Receptor (4) E1/E2/E3 Enzyme (1) EAAT (1) Endogenous Metabolite (5) ERK (6) GABA Receptor (20) GCGR (2) GLP Receptor (4) Guanylate Cyclase (1) Histone Methyltransferase (2) iGluR (7) Isotope-Labeled Compounds (5) mAChR (19) Melanocortin Receptor (6) mGluR (40) nAChR (9) NAMPT (1) Opioid Receptor (3) P-glycoprotein (1) Parasite (2) PERK (2) PINK1/Parkin (1) Reference Standards (6) Sigma Receptor (5) TRP Channel (1) Urotensin Receptor (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (4) Endocrinology (2) Infection (3) Inflammation/Immunology (13) Metabolic Disease (12) Neurological Disease (114)
Click Chemistry:	Alkynes (1)

145

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0106

Levamisole Maximum Cited Publications 14 Publications Verification (-)-Tetramisole	nAChR Parasite	Infection Inflammation/Immunology Cancer
Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC₅₀=300 μM) and α3β4 (EC₅₀=100 μM) subtype of nAChRs. Orally active .

HY-B1456A

Fenoprofen 2 Publications Verification LILLY-53858	COX Melanocortin Receptor ERK	Inflammation/Immunology
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .

HY-113320

Etiocholanolone 5β-Androsterone	GABA Receptor Endogenous Metabolite	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 GABA_A receptor than its enantiomer form .

HY-128770

LY3154207 2 Publications Verification	Dopamine Receptor	Neurological Disease
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀=3 nM) .

HY-169329

BIO-2007817	PINK1/Parkin E1/E2/E3 Enzyme	Neurological Disease
BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC₅₀: 0.17 μM) .

HY-18654

ADX88178 1 Publications Verification	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-129086

BPAM344	iGluR	Neurological Disease
BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM) .

HY-120613

BMS-986187	Opioid Receptor	Neurological Disease
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC₅₀ of 0.03 μM and a pK_B of 6.02 (～1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC₅₀=3 μM) .

HY-13058

ADX-47273 1 Publications Verification	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-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-120023

VU0453595 2 Publications Verification	mAChR	Neurological Disease
VU0453595 is a highly selective, systemically active M₁ positive allosteric modulator (PAM, EC₅₀=2140 nM) for the research of schizophrenia .

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-108340

PF-06767832	mAChR	Neurological Disease
PF-06767832 is a potent muscarinic M1 selective positive allosteric modulator (PAM), with the EC₅₀ of 60 nM. PF-06767832 has good brain penetration .

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-120530

JNJ-46281222	mGluR	Neurological Disease
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (K_d = 1.7 nM) and a high modulatory potency (pEC₅₀ = 7.71) .

HY-14612

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 .

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-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 K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-122819

Calindol hydrochloride	CaSR	Cardiovascular Disease
Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC₅₀ of 132 nM .

HY-141515

BMS-986121	Opioid Receptor	Neurological Disease
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs .

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification Tetrahydro-11-deoxycorticosterone-d₃	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-12149

A-867744	nAChR	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-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-114933

VU0119498 1 Publications Verification	mAChR	Neurological Disease Metabolic Disease
VU0119498 is a pan G_q 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-124821

VA012	5-HT Receptor	Neurological Disease Metabolic Disease
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT_2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .

HY-156331

VU6004909	mGluR	Neurological Disease
VU6004909 is a blood-brain barrier penetrated mGlu1* positive* allosteric modulator (PAM), with the EC₅₀s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .

HY-136190

TRPC6-PAM-C20	TRP Channel	Neurological Disease
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca ²⁺ concentrations ([Ca ²⁺]i) in TRPC6-expressing HEK293 cells with an EC₅₀ of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-107423

GNE 6901	iGluR	Neurological Disease
GNE 6901 (compound 40) is a potent GluN2A-selective NMDAR positive allosteric modulator (PAM) with an EC₅₀ of 382 nM .

HY-103571

VU0285683	mGluR	Neurological Disease
VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety .

HY-100605

VU0483605	mGluR	Others
VU0483605 is a potent and brain-penetrated mGlu₁ receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu₁ PAM activity at both human and rat, with EC₅₀ values of 390 and 356 nM, respectively .

HY-116463

E1R	Sigma Receptor	Neurological Disease
E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity .

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-143312D

(R)-V-0219 hydrochloride	GLP Receptor	Metabolic Disease
(R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R .

HY-162454

DA-023	EAAT	Neurological Disease
DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC₅₀ value of 1 nM .

HY-15476

VU 0364439	mGluR	Neurological Disease
VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

HY-121806

VU0486846	mAChR	Neurological Disease
VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .

HY-14419

TCN238	mGluR	Neurological Disease
TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC₅₀ of 1 μM .

HY-118416

BMS-986124	Opioid Receptor	Neurological Disease
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM) .

HY-118179

VU0486321	mGluR	Neurological Disease
VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.

HY-119078

VU0080241	mGluR	Neurological Disease
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC₅₀ of 4.6 μM .

HY-19623

VU0092273	mGluR	Neurological Disease
VU0092273 is a potent mGlu5 positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC₅₀ of 0.27 μM .

HY-144291

LY3154885	Dopamine Receptor	Neurological Disease
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .

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-117851

AC-265347	CaSR	Metabolic Disease Endocrinology
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pK_B) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .

HY-120004

PF-06827443	mAChR	Infection
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .

HY-126327

UNC4976	Histone Methyltransferase	Cancer
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-155628

AMPA receptor modulator-6	iGluR	Others
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .

HY-117611

GAT107	nAChR	Neurological Disease
GAT107 (compound 1b) is a potent α7 nAChR ago-PAMs (positive allosteric modulators) .

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-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-126327

UNC4976	Histone Methyltransferase	Cancer
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-P11258

UPG-108	Urotensin Receptor	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
UPG-108, a peptide compound, is a non-competitive allosteric modulator of Urotensin II receptors (UTR). UPG-108 significantly enhances the efficacy of UTR agonists but reduces the potency of UTR agonists. UPG-111 efficiently induces calcium release and does not cause contraction of rat aortic rings without endothelial denudation. UPG-111 can be used to study various diseases related to the angiotensinergic system .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113320

Etiocholanolone 5β-Androsterone	Microorganisms Endogenous metabolite Steroids Source Classification	GABA Receptor Endogenous Metabolite
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 GABA_A receptor than its enantiomer form .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification	GABA Receptor Endogenous Metabolite
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

Cat. No.	Product Name	Chemical Structure

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. 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-W777503

Calindol hydrochloride-13C,D2
Calindol hydrochloride- ¹³C,d₂ is the deuterium and ¹³C labeled Calindol hydrochloride (HY-122819). Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC₅₀ of 132 nM .

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. 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-173251S

ENX-101
ENX-101 is an orally active (GABA_A) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC₅₀ = 0.76 nM), α2β3γ2L (EC₅₀ = 0.61 nM), α3 (EC₅₀ = 1.97 nM), α5 (EC₅₀ = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .

HY-B1456AS

Fenoprofen-13C6 sodium hydrate

Fenoprofen- ¹³C₆ (LILLY-53858- ¹³C₆) sodium hydrate is the ¹³C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .

Cat. No.	Product Name		Classification

HY-118022

VU0361747		Alkynes
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .

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