MRGPRX4

Summary

MRGPRX4 (MAS related GPR family member X4, HGNC:17617) is a protein-coding gene on chromosome 11p15.1, encoding Mas-related G-protein coupled receptor member X4 (Q96LA9). G protein-coupled receptor for bile acids, which is specifically expressed in sensory neurons of dorsal root ganglion and is involved in itch perception.

Predicted to enable G protein-coupled receptor activity. Predicted to be involved in G protein-coupled receptor signaling pathway. Predicted to act upstream of or within chemosensory behavior and hematopoietic progenitor cell differentiation. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 117196 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 57 total
• Druggable target: yes
• MANE Select transcript: NM_054032

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17617
Approved symbol	MRGPRX4
Name	MAS related GPR family member X4
Location	11p15.1
Locus type	gene with protein product
Status	Approved
Aliases	MRGX4
Ensembl gene	ENSG00000179817
Ensembl biotype	protein_coding
OMIM	607230
Entrez	117196

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000314254

RefSeq mRNA: 1 — MANE Select: NM_054032 NM_054032

CCDS: CCDS7831

Canonical transcript exons

ENST00000314254 — 1 exons

Exon	Start	End
ENSE00001233154	18172837	18174280

Expression profiles

Bgee: expression breadth tissue_specific, 3 present calls, max score 59.68.

Top tissues by expression

225 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
esophagus squamous epithelium	UBERON:0006920	59.68	gold quality
amniotic fluid	UBERON:0000173	55.97	gold quality
buccal mucosa cell	CL:0002336	55.73	gold quality
nasal cavity epithelium	UBERON:0005384	53.97	gold quality
cartilage tissue	UBERON:0002418	53.14	gold quality
endothelial cell	CL:0000115	53.04	gold quality
vastus lateralis	UBERON:0001379	52.61	gold quality
mammary duct	UBERON:0001765	52.52	gold quality
quadriceps femoris	UBERON:0001377	52.33	gold quality
germinal epithelium of ovary	UBERON:0001304	51.98	gold quality
heart right ventricle	UBERON:0002080	51.61	gold quality
upper leg skin	UBERON:0004262	51.33	gold quality
trabecular bone tissue	UBERON:0002483	50.74	gold quality
skin of hip	UBERON:0001554	50.18	gold quality
pigmented layer of retina	UBERON:0001782	49.26	gold quality
Brodmann (1909) area 46	UBERON:0006483	49.19	gold quality
sperm	CL:0000019	48.09	gold quality
biceps brachii	UBERON:0001507	48.01	gold quality
gingiva	UBERON:0001828	45.65	gold quality
gingival epithelium	UBERON:0001949	45.14	gold quality
ventral tegmental area	UBERON:0002691	44.11	gold quality
adult organism	UBERON:0007023	43.76	gold quality
mammary gland	UBERON:0001911	43.75	gold quality
thoracic mammary gland	UBERON:0005200	43.58	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	43.37	gold quality
entorhinal cortex	UBERON:0002728	43.22	gold quality
nipple	UBERON:0002030	43.02	gold quality
secondary oocyte	CL:0000655	42.57	gold quality
mammalian vulva	UBERON:0000997	42.29	gold quality
layer of synovial tissue	UBERON:0007616	42.06	silver quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.98

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 7)

• data indicate that genetic variation in MRGPRX4 contributes to inter-individual and inter-ethnic differences in the preference for mentholated cigarettes. (PMID:30768591)
• data support a model whereby both bile acids and bilirubin contribute to cholestatic itch via agonism at MRGPRX4 (PMID:31068464)
• Taken together, these data strongly suggest that MRGPRX4 is a novel bile acid receptor that likely underlies cholestatic itch in human, providing a promising new drug target for anti-itch therapies. (PMID:31500698)
• MRGPRX4 in Cholestatic Pruritus. (PMID:34161994)
• Structure, function and pharmacology of human itch GPCRs. (PMID:34789874)
• Itch receptor MRGPRX4 interacts with the receptor activity-modifying proteins. (PMID:37003505)
• MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model. (PMID:38718132)

Cross-species orthologs

26 orthologs

Organism	Symbol	Gene ID
mus_musculus	Mrgprb2	ENSMUSG00000050425
mus_musculus	Mrgpra1	ENSMUSG00000050650
mus_musculus	Mrgprb8	ENSMUSG00000050870
mus_musculus	Mrgpra6	ENSMUSG00000052303
mus_musculus	Mrgpra4	ENSMUSG00000067173
mus_musculus	Mrgprb3	ENSMUSG00000070546
mus_musculus	Mrgprb1	ENSMUSG00000070547
mus_musculus	Mrgprb4	ENSMUSG00000070550
mus_musculus	Mrgprb5	ENSMUSG00000070551
mus_musculus	Mrgprx1	ENSMUSG00000070552
mus_musculus	Mrgprx2	ENSMUSG00000074109
mus_musculus	Mrgpra9	ENSMUSG00000074111
mus_musculus	Mrgpra3	ENSMUSG00000078698
mus_musculus	Mrgpra2a	ENSMUSG00000093973
mus_musculus	Mrgpra2b	ENSMUSG00000096719
rattus_norvegicus	Mrgprx3	ENSRNOG00000014227
rattus_norvegicus	Mrgprx1	ENSRNOG00000014242
rattus_norvegicus	Mrgprb3l	ENSRNOG00000014266
rattus_norvegicus	Mrgprb5	ENSRNOG00000022703
rattus_norvegicus	Mrgprx2l	ENSRNOG00000022729
rattus_norvegicus	Mrgprb3	ENSRNOG00000028982
rattus_norvegicus	Mrgprb4	ENSRNOG00000033021
rattus_norvegicus	Mrgprb2	ENSRNOG00000037156
rattus_norvegicus	Mrgprb13	ENSRNOG00000074277
rattus_norvegicus		ENSRNOG00000081169
rattus_norvegicus		ENSRNOG00000084911

Paralogs (10): MAS1 (ENSG00000130368), MRGPRX1 (ENSG00000170255), MRGPRF (ENSG00000172935), MRGPRD (ENSG00000172938), GPR152 (ENSG00000175514), MRGPRX3 (ENSG00000179826), MRGPRG (ENSG00000182170), MRGPRX2 (ENSG00000183695), MRGPRE (ENSG00000184350), MAS1L (ENSG00000204687)

Protein

Protein identifiers

Mas-related G-protein coupled receptor member X4 — Q96LA9 (reviewed: Q96LA9)

Alternative names: Sensory neuron-specific G-protein coupled receptor 5/6

All UniProt accessions (1): Q96LA9

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor for bile acids, which is specifically expressed in sensory neurons of dorsal root ganglion and is involved in itch perception. Activated by bile acids, such as deoxycholate, chenodeoxycholate, taurocholate, taurodeoxycholate and taurodeoxycholate. Has a preference for 3-sulfated bile acids, such as deoxycholate 3-sulfate, glycoursodeoxycholate 3-sulfate and tauroursodeoxycholate 3-sulfate, which are present at high level in cholestatic patients with itch symptoms. Bile acid-binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. MRGPRX4 is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca2+ ions from intracellular stores, respectively.

Subcellular location. Cell membrane.

Tissue specificity. Uniquely localized in a subset of small dorsal root and trigeminal sensory neurons.

Disease relevance. MRGPRX4 activation by high blood levels of bile salts in individuals with cholestasis is involved in the pathogenesis of chronic itch experienced by these patients.

Activity regulation. Bilirubin IXalpha facilites activation by acting as a positive allosteric modulator. Activated by nateglinide drug, a FDA approved drug for the treatment of diabetes, eliciting chronic itching (pruritus), a well-known side effect of nateglinide. Specifically activated by MS47134, a nateglinide analog. Activated by fospropofol, a sedative-hypnotic drug, eliciting chronic itching (pruritus), a well-known side effect of fospropofol. Menthol hampers activation by acting as a negative modulator.

Similarity. Belongs to the G-protein coupled receptor 1 family. Mas subfamily.

RefSeq proteins (1): NP_473373* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR026234	MRGPCRFAMILY	Family

Pfam: PF00001

UniProt features (65 total): mutagenesis site 14, helix 14, topological domain 8, transmembrane region 7, sequence variant 6, strand 5, turn 3, glycosylation site 2, disulfide bond 2, sequence conflict 2, chain 1, region of interest 1

Structure

Experimental structures (PDB)

7 structures.

PDB	Method	Resolution (Å)
9V82	ELECTRON MICROSCOPY	2.56
7S8P	ELECTRON MICROSCOPY	2.6
9V81	ELECTRON MICROSCOPY	2.63
9LRS	ELECTRON MICROSCOPY	2.83
8K4S	ELECTRON MICROSCOPY	2.9
8YRG	ELECTRON MICROSCOPY	3.14
8KEX	ELECTRON MICROSCOPY	3.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96LA9-F1	81.36	0.49

Antibody-complex structures (SAbDab): 3 — 7S8P, 8K4S, 8YRG

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Disulfide bonds (2): 23–251, 161–173

Glycosylation sites (2): 25, 89

Mutagenesis-validated functional residues (14):

Position	Phenotype
82	decreased binding to 3-sulfated bile acids. decreased activation by phosphate-modified drugs, such as fospropofol. decre
86	decreased binding to 3-sulfated bile acids. decreased activation by phosphate-modified drugs, such as fospropofol.
95	decreased binding to 3-sulfated bile acids. decreased activation by phosphate-modified drugs, such as fospropofol. decre
96	decreased binding to 3-sulfated bile acids. decreased activation by agonists.
99	decreased binding to 3-sulfated bile acids.
158	decreased activation by phosphate-modified drugs, such as fospropofol. decreased activation by agonists.
159	reduced affinity for deoxycholate ligand.
180	reduced affinity for deoxycholate ligand. increased localization to the plasma membrane.
232	decreased binding to 3-sulfated bile acids.
235	reduced affinity for deoxycholate and 3-sulfated bile acids.
240	decreased binding to 3-sulfated bile acids. decreased activation by agonists.
241	decreased binding to 3-sulfated bile acids.
250	decreased activation by phosphate-modified drugs, such as fospropofol.
254	decreased activation by phosphate-modified drugs, such as fospropofol.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 20 (showing top): MODULE_308, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_SENSORY_PERCEPTION, GOBP_PHOSPHOLIPASE_C_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, ACEVEDO_METHYLATED_IN_LIVER_CANCER_DN, GOBP_ADENYLATE_CYCLASE_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, MARTENS_TRETINOIN_RESPONSE_UP, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, TFEB_TARGET_GENES, GSE13485_DAY1_VS_DAY3_YF17D_VACCINE_PBMC_UP, GSE13485_DAY1_VS_DAY7_YF17D_VACCINE_PBMC_UP, TBX1_TARGET_GENES, GOBP_BILE_ACID_SIGNALING_PATHWAY

GO Biological Process (4): G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), sensory perception of itch (GO:0160025), signal transduction (GO:0007165)

GO Molecular Function (2): G protein-coupled receptor activity (GO:0004930), G protein-coupled bile acid receptor activity (GO:0038182)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	2
G protein-coupled receptor signaling pathway	2
signal transduction	1
phospholipase C activator activity	1
sensory perception	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
transmembrane signaling receptor activity	1
adenylate cyclase-activating G protein-coupled bile acid receptor signaling pathway	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

270 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MRGPRX4	NPFF	O15130	822
MRGPRX4	TRPA1	O75762	462
MRGPRX4	ARRB2	P32121	462
MRGPRX4	TAS2R38	P59533	448
MRGPRX4	GPBAR1	Q8TDU6	433
MRGPRX4	DCAF12L2	Q5VW00	397
MRGPRX4	TRPM8	Q7Z2W7	387
MRGPRX4	MORF4L2	Q15014	371
MRGPRX4	CIMIP2A	Q6J272	368
MRGPRX4	NR1H4	Q96RI1	336
MRGPRX4	NTS	P30990	334
MRGPRX4	PXDN	Q92626	333
MRGPRX4	PXDNL	A1KZ92	333
MRGPRX4	ARRB1	P49407	328
MRGPRX4	KLHL41	O60662	327

IntAct

10 interactions, top by confidence:

A	B	Type	Score
MRGPRX4	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	MRGPRX4	psi-mi:“MI:0915”(physical association)	0.400
MRGPRX4	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
MRGPRX4	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
MRGPRX4	ATP1A3	psi-mi:“MI:0914”(association)	0.350

BioGRID (5): ANKRD13D (Affinity Capture-MS), PTDSS2 (Affinity Capture-MS), SPG7 (Affinity Capture-MS), DNAJB4 (Affinity Capture-MS), ATP1A3 (Affinity Capture-MS)

ESM2 similar proteins: Q2LL16, Q3KNA1, Q3UG50, Q3UG61, Q4QXU0, Q4QXU2, Q4QXU3, Q4QXU4, Q4QXU5, Q4QXU6, Q4QXX9, Q5U9D9, Q645T2, Q645T7, Q645V2, Q645V8, Q645Z2, Q646A2, Q646C4, Q646D6, Q646F4, Q646F6, Q67ES0, Q6L786, Q7TN39, Q7TN41, Q7TN44, Q7TN45, Q7TN49, Q7TN50, Q86SM5, Q8CIP3, Q8R4G1, Q8TDS7, Q91WW2, Q91WW3, Q91WW4, Q91WW5, Q91ZB5, Q91ZB9

Diamond homologs: B9VR26, O55197, O88680, P04201, P12526, P23749, P30554, P35410, Q16581, Q2LL16, Q3KNA1, Q3UG50, Q3UG61, Q4QXU0, Q4QXU2, Q4QXU3, Q4QXU4, Q4QXU5, Q4QXU6, Q4QXX9, Q5REI5, Q5U9D9, Q6L786, Q6TAC8, Q6XKD3, Q7TN38, Q7TN39, Q7TN40, Q7TN41, Q7TN44, Q7TN45, Q7TN49, Q7TN50, Q7TN51, Q86SM5, Q8CIP3, Q8NGA4, Q8R4G1, Q8TDS7, Q8VCJ6

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

57 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	46
Likely benign	7
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

282 predictions. Top by Δscore:

Variant	Effect	Δscore
11:18173097:TTTGG:T	donor_loss	1.0000
11:18173098:TTGGT:T	donor_loss	1.0000
11:18173099:TGG:T	donor_loss	1.0000
11:18173100:GGTA:G	donor_loss	1.0000
11:18173101:G:GG	donor_gain	1.0000
11:18173101:GT:G	donor_loss	1.0000
11:18173102:T:A	donor_loss	1.0000
11:18173582:GCC:G	donor_gain	1.0000
11:18173096:CTTTG:C	donor_gain	0.9900
11:18173097:TTTG:T	donor_gain	0.9900
11:18173098:TTG:T	donor_gain	0.9900
11:18173493:GATTA:G	donor_gain	0.9900
11:18173581:GGCC:G	donor_gain	0.9900
11:18173678:T:TA	donor_gain	0.9900
11:18173839:AGCCT:A	acceptor_gain	0.9900
11:18173840:GCCTG:G	acceptor_gain	0.9900
11:18173099:TG:T	donor_gain	0.9800
11:18173100:GG:G	donor_gain	0.9800
11:18173230:AG:A	acceptor_gain	0.9800
11:18173231:GG:G	acceptor_gain	0.9800
11:18173560:A:AG	donor_gain	0.9800
11:18173713:T:G	donor_gain	0.9800
11:18173840:GCCT:G	acceptor_gain	0.9800
11:18173227:CCCA:C	acceptor_loss	0.9700
11:18173228:CCAG:C	acceptor_loss	0.9700
11:18173229:CAG:C	acceptor_loss	0.9700
11:18173588:G:GG	donor_gain	0.9700
11:18173717:G:GG	donor_gain	0.9700
11:18173730:G:GT	donor_gain	0.9700
11:18173230:AGG:A	acceptor_gain	0.9600

AlphaMissense

2078 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:18173929:T:C	F225L	0.963
11:18173931:C:A	F225L	0.963
11:18173931:C:G	F225L	0.963
11:18173596:A:C	S114R	0.952
11:18173598:C:A	S114R	0.952
11:18173598:C:G	S114R	0.952
11:18173605:A:C	S117R	0.950
11:18173607:C:A	S117R	0.950
11:18173607:C:G	S117R	0.950
11:18173839:A:C	S195R	0.946
11:18173841:C:A	S195R	0.946
11:18173841:C:G	S195R	0.946
11:18174052:A:C	S266R	0.924
11:18174054:T:A	S266R	0.924
11:18174054:T:G	S266R	0.924
11:18173587:A:C	S111R	0.912
11:18173589:T:A	S111R	0.912
11:18173589:T:G	S111R	0.912
11:18173485:A:C	S77R	0.881
11:18173487:C:A	S77R	0.881
11:18173487:C:G	S77R	0.881
11:18173695:T:A	W147R	0.867
11:18173695:T:C	W147R	0.867
11:18173472:C:A	D72E	0.858
11:18173472:C:G	D72E	0.858
11:18174049:A:C	S265R	0.853
11:18174051:T:A	S265R	0.853
11:18174051:T:G	S265R	0.853
11:18173479:T:C	F75L	0.852
11:18173481:C:A	F75L	0.852

dbSNP variants (sampled 300 via entrez): RS1000939021 (11:18174447 A>G,T), RS1001267766 (11:18170870 A>G,T), RS1001579204 (11:18171077 A>G), RS1002843211 (11:18172355 C>A,G,T), RS1004067898 (11:18172494 G>A), RS1005072010 (11:18171183 C>A,T), RS1007310559 (11:18174416 G>T), RS1011560232 (11:18171825 G>A), RS1013171546 (11:18172399 G>A,C), RS1013383181 (11:18174452 A>C), RS1013869639 (11:18174733 G>A,C), RS1015241638 (11:18172496 T>C), RS1015468852 (11:18172695 C>T), RS1017114962 (11:18173639 T>C), RS1018330606 (11:18173956 A>G)

Disease associations

OMIM: gene MIM:607230 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523430 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Class A Orphans with emerging pharmacology

ChEMBL bioactivities

275 potent at pChembl≥5 of 275 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.52	IC50	3	nM	CHEMBL4878726
8.30	IC50	5	nM	CHEMBL4874540
8.30	IC50	5	nM	CHEMBL4850889
8.22	IC50	6	nM	CHEMBL4855031
8.22	IC50	6	nM	CHEMBL4878726
8.22	IC50	6	nM	CHEMBL4874540
8.22	IC50	6	nM	CHEMBL4848977
8.15	IC50	7	nM	CHEMBL4867400
8.15	IC50	7	nM	CHEMBL4874540
8.15	IC50	7	nM	CHEMBL4878726
8.15	IC50	7	nM	CHEMBL4850889
8.15	IC50	7	nM	CHEMBL4858820
8.10	IC50	8	nM	CHEMBL4878726
8.10	IC50	8	nM	CHEMBL4874540
8.05	IC50	9	nM	CHEMBL4871722
8.05	IC50	9	nM	CHEMBL4850889
8.00	IC50	10	nM	CHEMBL4850889
8.00	IC50	10	nM	CHEMBL4848977
8.00	IC50	10	nM	CHEMBL4878726
7.96	IC50	11	nM	CHEMBL4855031
7.96	IC50	11	nM	CHEMBL4850889
7.92	IC50	12	nM	CHEMBL4852609
7.89	IC50	13	nM	CHEMBL4867400
7.89	IC50	13	nM	CHEMBL4871722
7.85	IC50	14	nM	CHEMBL4855031
7.82	IC50	15	nM	CHEMBL4875180
7.82	IC50	15	nM	CHEMBL4875642
7.80	IC50	16	nM	CHEMBL4875642
7.80	IC50	16	nM	CHEMBL4858820
7.80	IC50	16	nM	CHEMBL4859372
7.80	IC50	16	nM	CHEMBL4855031
7.80	IC50	16	nM	CHEMBL4877820
7.77	IC50	17	nM	CHEMBL4852609
7.77	IC50	17	nM	CHEMBL4871722
7.77	IC50	17	nM	CHEMBL4870947
7.77	IC50	17	nM	CHEMBL4858820
7.70	IC50	20	nM	CHEMBL4859372
7.70	IC50	20	nM	CHEMBL4875180
7.70	IC50	20	nM	CHEMBL4867400
7.68	IC50	21	nM	CHEMBL4875642
7.68	IC50	21	nM	CHEMBL4877820
7.68	IC50	21	nM	CHEMBL4871722
7.68	IC50	21	nM	CHEMBL4858820
7.68	IC50	21	nM	CHEMBL4867400
7.66	IC50	22	nM	CHEMBL4855031
7.66	IC50	22	nM	CHEMBL4875642
7.66	IC50	22	nM	CHEMBL4852609
7.64	IC50	23	nM	CHEMBL4848977
7.64	IC50	23	nM	CHEMBL4855031
7.64	IC50	23	nM	CHEMBL4871722

CTD chemical–gene interactions

6 total (human), top 6 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	increases methylation, affects cotreatment	1
Resveratrol	affects cotreatment, decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Leflunomide	increases expression	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Plant Extracts	affects cotreatment, decreases expression	1

ChEMBL screening assays

15 unique, capped per target: 13 functional, 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4420050	Functional	Antagonist activity at recombinant human MrgprX4 expressed in HEK293 cells assessed as blockade of bilirubin-induced inositol phosphate accumulation incubated for 1 hr at at 37 degC followed by incubation for 30 mins at room temperature bef	Compositions and methods for treating g protein coupled receptor mediated conditions
CHEMBL4883538	Binding	PRESTO-Tango GPCRome screening (MRGPRX4)	Data for DCP probe UCSF924

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_KY50	PathHunter CHO-K1 MRGPRX4 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.