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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Mas-related G-protein coupled receptor member X2

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
19
Compounds
3
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

MRGX2_HUMANMRGPRX2Homo sapiens

Mas-related G protein-coupled receptor member X2

Mast cell-specific G protein-coupled receptor for basic secretagogues, which regulates mast cell degranulation and itch-related hypersensitivity reactions22069323,25517090,28288109,34789874,34789875. A secretagogue is an agent that promotes the secretion of hormones, neurohormones, chemical neurotransmitters or other compounds synthesized and secreted by cells25517090. Basic secretagogues comprise a set of cationic amphiphilic drugs, as well as endo- or exogenous peptides, consisting of a basic head group and a hydrophobic core25517090. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase28288109,34789874,34789875. MRGPRX2 is both coupled to G(q) and G(i) G proteins: G(q) coupling activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers, while G(i) coupling mediates inhibition of adenylate cyclase activity28288109,34789874,34789875. Recognizes and binds small molecules containing a cyclized tetrahydroisoquinoline (THIQ), such as non-steroidal neuromuscular blocking drugs (NMBDs), including tubocurarine and atracurium (By similarity). In response to these compounds, mediates pseudo-allergic reactions characterized by histamine release, inflammation and airway contraction (By similarity). Acts as a receptor for substance P, a basic secretagogue neuropeptide released from the terminals of specific sensory nerves, initiating a signaling that mediates neurogenic inflammation and pain30686732,34789875. Neurogenic inflammation includes mast cell activation, recruitment of immune cells and release of inflammatory mediators, such as cytokines and chemokines (By similarity). The inflammatory response can then activate or sensitize nociceptors, promoting pain (By similarity). Acts as a receptor for a number of other ligands, including peptides and alkaloids, such as cortistatin-14, proadrenomedullin peptides PAMP-12 and, at lower extent, PAMP-20, antibacterial protein LL-37, PMX-53 peptide, beta-defensins, complanadine A and CXCL1712915402,15823563,21441599,22069323,23698749,24930830,34789874,34789875. Also acts as a receptor for opioids, such as (-)- and (+)-morphine, hydrocodone, sinomenine, dextromethorphan, dynorphin A, dynorphin B, and alpha- and beta-neoendorphin, promoting mast cell degranulation28288109

Quoted from UniProt’s FUNCTION annotation for Q96LB1 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
CORT0.9960.9000.0000.968
CAMP0.9760.0000.0000.976
ADM0.9340.9000.0000.373
GNAI10.9030.9000.0000.071
GNAS0.9010.9000.0000.052
GNB10.9000.9000.0000.000
CENPS-CORT0.9000.9000.0000.000
TAC10.8880.0000.0000.888
NPFF0.8520.0000.0000.852
GNG20.8000.8000.0000.000

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Mast cells13.8 nCPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — no resolved target expressed herecerebellum — no resolved target expressed herehippocampal formation — no resolved target expressed hereamygdala — no resolved target expressed herehypothalamus — no resolved target expressed herethalamus — no resolved target expressed herebasal ganglia — no resolved target expressed heremedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Body

heart — no resolved target expressed heresmooth muscle — no resolved target expressed herelung — 0.1 nTPM, from MRGPRX2liver — no resolved target expressed herekidney — no resolved target expressed herestomach — no resolved target expressed hereduodenum — no resolved target expressed heresmall intestine — 0.1 nTPM, from MRGPRX2colon — 0.1 nTPM, from MRGPRX2adrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — no resolved target expressed hereurinary bladder — 0.5 nTPM, from MRGPRX2skeletal muscle — no resolved target expressed herespleen — no resolved target expressed heresalivary gland — 0.1 nTPM, from MRGPRX2
01 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of MRGPRX2 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Peripheral and autonomic · 5

  • urinary bladder0.5 nTPM
  • lung0.1 nTPM
  • small intestine0.1 nTPM
  • colon0.1 nTPM
  • salivary gland0.1 nTPM

Transcript is not protein. These are RNA levels for MRGPRX2, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 6

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665199
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665199
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665199
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665202
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665202
Mas-related G-protein coupled receptor member X2Other named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665202

Other measurements 13

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Mas-related G-protein coupled receptor member X2Other named receptorspEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665199
Mas-related G-protein coupled receptor member X2Other named receptorspEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665202
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665206
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665206
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665206
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665207
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665207
Mas-related G-protein coupled receptor member X2Other named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665207
Mas-related G-protein coupled receptor member X2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665208
Mas-related G-protein coupled receptor member X2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665208
Mas-related G-protein coupled receptor member X2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665209
Mas-related G-protein coupled receptor member X2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665209
Mas-related G-protein coupled receptor member X2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5665255
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