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Results for "

positive allosteric modulator (PAM)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adenosine Receptor (4) Cannabinoid Receptor (3) CaSR (3) Cholinesterase (ChE) (1) Cytochrome P450 (2) Dopamine Receptor (2) E1/E2/E3 Enzyme (1) EAAT (2) Endogenous Metabolite (5) GABA Receptor (12) GCGR (2) GLP Receptor (6) Guanylate Cyclase (1) Histone Methyltransferase (2) iGluR (5) Isotope-Labeled Compounds (2) mAChR (14) mGluR (34) nAChR (6) NAMPT (2) Opioid Receptor (3) P-glycoprotein (1) Parasite (2) PERK (1) PINK1/Parkin (1) Sigma Receptor (5) TRP Channel (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (2) Endocrinology (2) Infection (3) Inflammation/Immunology (4) Metabolic Disease (12) Neurological Disease (86)
Click Chemistry:	Alkynes (1)

115

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15476

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

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-162455

NA-014	EAAT	Others
NA-014 (40) is a selective EAAT2 positive allosteric modulator (PAM), with an EC₅₀ of 3 nM .

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-14419

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

HY-121806

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

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-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-103535

GBLD345	GABA Receptor	Neurological Disease
GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .

HY-159509

Claziprotamidum Claziprotamide	Others	Others
Claziprotamidum (Claziprotamide) is a pantothenate kinases 1 and 3 (PanK1 and PanK3) positive allosteric modulator (PAM) .

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	Others	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-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-155467

MRS7935	Adenosine Receptor	Endocrinology
MRS7935 (compound 15) is an A1AR positive allosteric modulator (PAM) with an EC₅₀ of approximately 2 μM .

HY-117611

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

HY-159177

M4 mAChR Modulator-1	mAChR	Neurological Disease
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .

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-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-137204

COR659	GABA Receptor	Neurological Disease
COR659 is a potent and effective GABA_B positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats .

HY-16951

VU-1545	mGluR	Neurological Disease
VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a K_i of 156 nM and an EC₅₀ of 9.6 nM .

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-129086

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

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-128770

LY3154207 1 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-132806

Alogabat RG-7816; RO-7017773	GABA Receptor	Neurological Disease
Alogabat (example 8) is a GABA_A α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .

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-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-168025

VU6007496	Others	Neurological Disease
VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .

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-120023

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

HY-122164

LY-503430	iGluR	Neurological Disease
LY-503430 is an orally active AMPA receptor positive allosteric modulator (PAM). LY-503430 can be used for the study of Parkinson's disease .

HY-161810

MRS8247	Adenosine Receptor	Others
MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists .

HY-123667

NCFP	mGluR	Neurological Disease
NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases .

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-118022

VU0361747	mGluR	Neurological Disease
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 .

HY-117408

VU6004256	mAChR	Neurological Disease
VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC₅₀ value of 155 nM. VU6004256 has the potential 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-160529

α7 nAChR Modulator-2	nAChR	Neurological Disease
α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an *EC₅₀ of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders .*

HY-128783

VU0090157	mAChR	Neurological Disease
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .

HY-124372

JNJ-46356479	mGluR	Neurological Disease
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC₅₀ of 78 nM. JNJ-46356479 shows active in vivo .

HY-161113

Z8554052021	CaSR	Metabolic Disease
Z8554052021 (compound 2021) is a potent CaSR and indeed GPCR positive allosteric modulator (PAM) with an EC₅₀ of 3.3 nM. Z8554052021 has the potential for hyperparathyroidism research .

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-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-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-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-162662

VU6008677	Cytochrome P450 mAChR	Neurological Disease
VU6008677 is a positive allosteric modulator (PAM) for M4, with EC₅₀ of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .

HY-159624

KK-92A	GABA Receptor	Neurological Disease
KK-92A, a blood-brain barrier penetrated GABAB positive allosteric modulator (PAM), suppresses alcohol self-administration and cue-induced reinstatement of alcohol seeking in rats .

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[1][2][3].

HY-119772

VU0366369 ML137	Cholinesterase (ChE)	Neurological Disease
VU0366369 (ML137) is a selective positive allosteric modulator (PAM) for mAChR M1 with an EC₅₀ of 830 nM. VU0366369 can be used in research about central nervous system diseases .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

194 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 194 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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113346

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

HY-113320

Etiocholanolone 5β-Androsterone	Structural Classification Microorganisms Source classification Endogenous metabolite Steroids	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 .

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[1][2][3].

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

Cat. No.	Product Name		Classification