Tchem P2RX4 P2X purinoceptor 4

Protein Summary

Description

Receptor for ATP that acts as a ligand-gated ion channel. This receptor is insensitive to the antagonists PPADS and suramin. The product of this gene belongs to the family of purinoceptors for ATP. This receptor functions as a ligand-gated ion channel with high calcium permeability. The main pharmacological distinction between the members of the purinoceptor family is the relative sensitivity to the antagonists suramin and PPADS. The product of this gene has the lowest sensitivity for these antagonists. Multiple alternatively spliced transcript variants, some protein-coding and some not protein-coding, have been found for this gene. [provided by RefSeq, Feb 2012]

Uniprot Accession IDs

• Q99571
• E7EPF7
• F6RU17
• O00450
• O14722
• Q5U089
• Q5U090
• Q8N4N1
• Q9UBG9
• P2X4

Gene Name

• P2RX4

Ensembl ID

• ENST00000337233
• ENSP00000336607
• ENSG00000135124
• ENST00000359949
• ENSP00000353032
• ENST00000542067
• ENSP00000438329

Symbol

• P2X4
• P2X4R

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
biological process	0.96
cellular component	0.88
transcription factor perturbation	0.84
histone modification site profile	0.75

Protein Classes

DTO Classes

Protein / Ion Channel / Atp-gated P2x Receptor Cation Channel (P2x Receptor) Family / P2x Purinoceptor 4

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 480.62   (req: < 5)

Gene RIFs: 53   (req: <= 3)

Antibodies: 240   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 480.62   (req: >= 5)

Gene RIFs: 53   (req: > 3)

Antibodies: 240   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 47

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 90

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 2

Expression Data (0 Tissues)

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No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (4)

Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (2)

Explore Approved Drugs

1 – 2 of 2

adenosine triphosphate

P2RX4Tchem IC

AGONIST pEC50 : 6.3

paroxetine

P2RX4Tchem IC

INHIBITOR pKi : 10.4

Active Ligands (90)

Explore Active Ligands

1 – 10 of 90

Ap4A

P2RX4Tchem IC

pEC50 : 6.74

2MeSATP

P2RX4Tchem IC

-log(-) : 7.7

PPADS

P2RX4Tchem IC

pIC50 : 6.62

TNP-ATP

P2RX4Tchem IC

pKi : 7.31

Bz-ATP

P2RX4Tchem IC

pEC50 : 8.7

N-(3,5-Bis(trifluoromethyl)phenyl)-1-hydroxy-2-naphthamide

P2RX4Tchem IC

pIC50 : 6.71

10-Benzyl-9-phenyl-9,10-dihydroacridin-9-ol

P2RX4Tchem IC

pIC50 : 6.37

CHEMBL4640175

P2RX4Tchem IC

pIC50 : 7.5

N-(3,5-Bis(trifluoromethyl)phenyl)-3-chloro-2-hydroxybenzamide

P2RX4Tchem IC

pIC50 : 7.31

5-Chloro-N-(3-chlorophenyl)-2-hydroxybenzamide

P2RX4Tchem IC

pIC50 : 7.12

Protein-Protein Interactions (84)

Explore Interacting Targets

1 – 10 of 84

• See Interactions on String-DB

CYBC1

Tdark

Novelty:  0.72567331

p_int:  0.999979184

p_ni:  0.000020769

p_wrong:  4.7e-8

Score:  0.235

Data Source:  BioPlex,STRINGDB

B3GALT5

Tbio

Family:  Enzyme

Novelty:  0.04158039

p_int:  0.999968548

p_ni:  0.000031318

p_wrong:  1.34e-7

Data Source:  BioPlex

SPPL2B

Tchem

Family:  Enzyme

Novelty:  0.0274774

p_int:  0.999903309

p_ni:  0.000096569

p_wrong:  1.22e-7

Data Source:  BioPlex

FAM20B

Tdark

Family:  Enzyme

Novelty:  0.07347685

p_int:  0.999499577

p_ni:  0.000500417

p_wrong:  6e-9

Score:  0.518

Data Source:  BioPlex,STRINGDB

PIGH

Tbio

Family:  Enzyme

Novelty:  0.0584561

p_int:  0.999040372

p_ni:  0.00084138

p_wrong:  0.000118248

Score:  0.235

Data Source:  BioPlex,STRINGDB

CSGALNACT2

Tbio

Family:  Enzyme

Novelty:  0.0770692

p_int:  0.998733181

p_ni:  0.00036208

p_wrong:  0.000904739

Data Source:  BioPlex

EIF2B3

Tbio

Novelty:  0.04963646

p_int:  0.996952978

p_ni:  0.003047022

Data Source:  BioPlex

EIF2B5

Tbio

Novelty:  0.0102209

p_int:  0.993729264

p_ni:  0.006270736

Score:  0.196

Data Source:  BioPlex,STRINGDB

TNPO3

Tbio

Novelty:  0.01709028

p_int:  0.968982129

p_ni:  0.031017871

Data Source:  BioPlex

EIF2B4

Tbio

Novelty:  0.05080792

p_int:  0.958370796

p_ni:  0.041629204

Data Source:  BioPlex

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (6)

Reactome (4)

KEGG (2)

Elevation of cytosolic Ca2+ levels (R-HSA-139853)

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1 – 4 of 4

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Elevation of cytosolic Ca2+ levels	16 targets	R-HSA-139853
Reactome	Hemostasis	666 targets	R-HSA-109582
Reactome	Platelet calcium homeostasis	28 targets	R-HSA-418360
Reactome	Platelet homeostasis	88 targets	R-HSA-418346

Name	Explore in Pharos	Explore in Source
Elevation of cytosolic Ca2+ levels	16 targets	R-HSA-139853
Hemostasis	666 targets	R-HSA-109582
Platelet calcium homeostasis	28 targets	R-HSA-418360
Platelet homeostasis	88 targets	R-HSA-418346

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (61)

Functions (10)

Components (14)

Processes (37)

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1 – 10 of 10

GO Term	Evidence	Assigned by
extracellularly ATP-gated cation channel activity	Inferred from Direct Assay (IDA)	UniProtKB
ligand-gated calcium channel activity	Inferred from Direct Assay (IDA)	BHF-UCL
purinergic nucleotide receptor activity	Inferred from Direct Assay (IDA)	BHF-UCL
cadherin binding	Inferred from Physical Interaction (IPI)	BHF-UCL
ATP-gated ion channel activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
copper ion binding	Inferred from Sequence or structural Similarity (ISS)	BHF-UCL
signaling receptor binding	Inferred from Sequence or structural Similarity (ISS)	BHF-UCL
zinc ion binding	Inferred from Sequence or structural Similarity (ISS)	BHF-UCL
protein homodimerization activity	Non-traceable Author Statement (NAS)	BHF-UCL
ATP binding	Inferred by Curator (IC)	BHF-UCL

Disease Associations (null)

No disease associations found

GWAS Traits (7)

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5

1 – 5 of 7

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
C-reactive protein measurement	EFO_0004458	2	22	23		98.6
serum gamma-glutamyl transferase measurement	EFO_0004532	1	11	11		98.4
IGF-1 measurement	EFO_0004627	1	2	2		83.8
body mass index	EFO_0004340	2	1	2		52
type II diabetes mellitus	EFO_0001360	1	1	0	1.1	15.8

• Explore on Target Illumination GWAS Analytics (TIGA)

Items per page:

5

1 – 5 of 7

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
C-reactive protein measurement	EFO_0004458	23		98.6
serum gamma-glutamyl transferase measurement	EFO_0004532	11		98.4
IGF-1 measurement	EFO_0004627	2		83.8
body mass index	EFO_0004340	2		52
type II diabetes mellitus	EFO_0001360	0	1.1	15.8

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UniProt Keyword Find Similar Targets

No Header	No Header
Alternative splicing
Complete proteome
Disulfide bond
Glycoprotein
Ion channel
Ion transport
Ligand-gated ion channel
Membrane
Polymorphism
Receptor

GWAS Trait Find Similar Targets

No Header	No Header
birth weight
body mass index
C-reactive protein measurement
IGF-1 measurement
schizophrenia
serum gamma-glutamyl transferase measurement
type II diabetes mellitus

MGI Phenotype Find Similar Targets

No Header	No Header
cardiovascular system phenotype
hematopoietic system phenotype
homeostasis/metabolism phenotype
immune system phenotype
muscle phenotype
nervous system phenotype
renal/urinary system phenotype
skeleton phenotype

IDG Resources

No IDG generated resources found

Orthologs (13)

1 – 5 of 13

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	purinergic receptor P2X 4	VGNC:8487	452319
Macaque	purinergic receptor P2X 4		702536
Mouse	purinergic receptor P2X, ligand-gated ion channel 4	MGI:1338859	18438
Rat	purinergic receptor P2X 4	RGD:62073	29659
Dog	purinergic receptor P2X 4	VGNC:44210	448783

Species	Name	OMA	EggNOG	Inparanoid
Chimp	purinergic receptor P2X 4
Macaque	purinergic receptor P2X 4
Mouse	purinergic receptor P2X, ligand-gated ion channel 4
Rat	purinergic receptor P2X 4
Dog	purinergic receptor P2X 4

Publication Statistics

PubMed Score 480.62

PubMed score by year

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PubTator Score 162.68

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Patents

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Related Publications

Text Mined References (76)

GeneRif Annotations (53)

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PMID	Year	Title