P2RX7

Summary

P2RX7 (purinergic receptor P2X 7, HGNC:8537) is a protein-coding gene on chromosome 12q24.31, encoding P2X purinoceptor 7 (Q99572). ATP-gated nonselective transmembrane cation channel that requires high millimolar concentrations of ATP for activation.

The product of this gene belongs to the family of purinoceptors for ATP. This receptor functions as a ligand-gated ion channel and is responsible for ATP-dependent lysis of macrophages through the formation of membrane pores permeable to large molecules. Activation of this nuclear receptor by ATP in the cytoplasm may be a mechanism by which cellular activity can be coupled to changes in gene expression. Multiple alternatively spliced variants have been identified, most of which fit nonsense-mediated decay (NMD) criteria.

Source: NCBI Gene 5027 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 96 total
• Druggable target: yes — 9 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002562

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8537
Approved symbol	P2RX7
Name	purinergic receptor P2X 7
Location	12q24.31
Locus type	gene with protein product
Status	Approved
Aliases	P2X7, MGC20089
Ensembl gene	ENSG00000089041
Ensembl biotype	protein_coding
OMIM	602566
Entrez	5027

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 11 nonsense_mediated_decay, 3 protein_coding, 1 retained_intron

ENST00000261826, ENST00000328963, ENST00000535250, ENST00000535600, ENST00000535928, ENST00000537312, ENST00000538011, ENST00000539606, ENST00000539695, ENST00000541022, ENST00000541564, ENST00000541716, ENST00000545434, ENST00000903311, ENST00000903312

RefSeq mRNA: 1 — MANE Select: NM_002562 NM_002562

CCDS: CCDS9213

Canonical transcript exons

ENST00000328963 — 13 exons

Exon	Start	End
ENSE00001319811	121184305	121188032
ENSE00002217016	121132876	121133095
ENSE00003466686	121175388	121175478
ENSE00003479632	121165357	121165437
ENSE00003488329	121166058	121166187
ENSE00003504884	121180354	121180455
ENSE00003521714	121177147	121177212
ENSE00003524359	121167488	121167624
ENSE00003554665	121162424	121162520
ENSE00003555907	121154785	121154953
ENSE00003604064	121156079	121156147
ENSE00003657849	121177297	121177446
ENSE00003721999	121160902	121160974

Expression profiles

Bgee: expression breadth ubiquitous, 243 present calls, max score 95.32.

FANTOM5 (CAGE): breadth broad, TPM avg 4.2416 / max 179.4347, expressed in 597 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
128396	4.1637	597
128395	0.0780	28

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
inferior vagus X ganglion	UBERON:0005363	95.32	gold quality
endothelial cell	CL:0000115	95.17	gold quality
corpus callosum	UBERON:0002336	94.56	gold quality
monocyte	CL:0000576	91.23	gold quality
subthalamic nucleus	UBERON:0001906	90.93	gold quality
mononuclear cell	CL:0000842	90.31	gold quality
leukocyte	CL:0000738	89.74	gold quality
superior vestibular nucleus	UBERON:0007227	88.88	gold quality
ventral tegmental area	UBERON:0002691	88.85	gold quality
globus pallidus	UBERON:0001875	88.82	gold quality
medial globus pallidus	UBERON:0002477	88.41	gold quality
cranial nerve II	UBERON:0000941	88.36	gold quality
substantia nigra pars reticulata	UBERON:0001966	87.43	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	87.40	gold quality
lateral globus pallidus	UBERON:0002476	87.03	gold quality
spinal cord	UBERON:0002240	86.96	gold quality
primary visual cortex	UBERON:0002436	86.24	gold quality
Brodmann (1909) area 23	UBERON:0013554	86.17	gold quality
occipital lobe	UBERON:0002021	86.15	gold quality
germinal epithelium of ovary	UBERON:0001304	85.59	gold quality
sural nerve	UBERON:0015488	85.13	gold quality
dorsal plus ventral thalamus	UBERON:0001897	84.59	gold quality
skin of hip	UBERON:0001554	84.52	gold quality
granulocyte	CL:0000094	84.37	gold quality
Ammon’s horn	UBERON:0001954	84.25	gold quality
trigeminal ganglion	UBERON:0001675	84.12	gold quality
medulla oblongata	UBERON:0001896	83.59	gold quality
parietal lobe	UBERON:0001872	83.25	gold quality
midbrain	UBERON:0001891	83.10	gold quality
middle temporal gyrus	UBERON:0002771	83.08	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-CURD-88	yes	49.83
E-MTAB-6678	yes	10.20
E-ANND-3	yes	9.84
E-GEOD-100618	no	214.07

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SP1

miRNA regulators (miRDB)

66 targeting P2RX7, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-150-5P	99.99	66.69	1976
HSA-MIR-4715-3P	99.98	66.03	670
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-7845-5P	99.88	64.88	771
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-26A-5P	99.78	73.52	2303
HSA-MIR-26B-5P	99.78	73.51	2305
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-3680-3P	99.75	72.51	3095
HSA-MIR-466	99.67	70.85	2863
HSA-MIR-6513-3P	99.59	69.77	1102
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-1275	99.47	67.90	2749
HSA-MIR-1324	99.46	66.57	1302
HSA-MIR-19A-5P	99.36	66.93	1675
HSA-MIR-19B-1-5P	99.36	67.07	1669
HSA-MIR-19B-2-5P	99.36	67.07	1669
HSA-MIR-125A-5P	99.36	70.59	1640
HSA-MIR-125B-5P	99.36	70.36	1662
HSA-MIR-133A-5P	99.28	69.13	941
HSA-MIR-3064-5P	99.26	66.13	1497
HSA-MIR-3085-3P	99.26	66.16	1490
HSA-MIR-6504-5P	99.26	65.95	1487
HSA-MIR-6852-5P	99.17	66.69	2073
HSA-MIR-6504-3P	99.17	69.31	2891
HSA-MIR-548AS-3P	99.12	69.12	2294

Literature-anchored findings (GeneRIF, showing 40)

• First description of the expression of functional P2X7 receptors in a subpopulation of osteoblasts, activation of which can result in ATP-mediated apoptosis. (PMID:11341329)
• K193 and K311 are essential residues in ATP binding in the hP2X(7)R. (PMID:11852049)
• loss-of-function polymorphic mutation has anti-apoptotic effect, resulting in increase in B-cell numbers in CLL (chronic lymphocytic leukemia) (PMID:11943260)
• The data show that monocyte-derived DC express the P2X7 receptor whose activation opens a cation-selective channel, and which leads to rapid and near complete shedding of CD23 (PMID:12456589)
• a loss-of-function polymorphism within the P2X(7) receptor: Ile-568 is critical to the trafficking domain, which is between residues 551 and 581. (PMID:12586825)
• detection of nonfunctional receptors in HEK293 cells and B-lymphocytes (PMID:12633871)
• P2X7R activation signals distinct, novel plasma membrane blebbing events (dependent on RhoA activation and Rho-effector kinase activity) and simultaneously initiates release of IL-1 beta. (PMID:12759456)
• Different purinergic receptors have different functional roles in human epidermis with P2Y1 and P2Y2 receptors controlling proliferation, while P2X5 and P2X7 receptors control early differentiation, terminal differentiation and death of keratinocytes. (PMID:12787128)
• The data presented are supportive of a model wherein residues Arg578 and Lys579 within the distal C-terminal lipid interaction domain of P2X7 are required for normal trafficking of the receptor as well as ligand binding and channel gating. (PMID:12874219)
• Blockade of the pore-forming P2X7 receptor inhibits formation of multinucleated human osteoclasts in vitro. (PMID:12874700)
• Non-melanoma skin cancers express functional purinergic receptors and that P2X7 receptor agonists significantly reduce cell numbers in vitro. (PMID:12880424)
• the influenceof P2X7 genotype on susceptibility to chronic lymphocytic leukaemia or clinical outcome is small (PMID:12931211)
• A single nucleotide polymorphism (1513A–>C) in the P2X7 gene allows survival of mycobacteria within infected host cells. (PMID:14607949)
• Activation of P2X(7) ionotropic receptors is necessary and sufficient to increase 2-arabinoylglycerol production in microglial cells. (PMID:14976257)
• ATP-induced release of IL-1 beta is slower in monocytes from subjects homozygous for the Glu496Ala loss-of-function polymorphism in the P2X7 receptor, and this reduced rate of IL-1 beta release is associated with a lower ATP-induced potassium ion efflux. (PMID:15004138)
• Our data do not support a role of the P2X7 genotype as a prognostic marker in B-cell CLL. (PMID:15089763)
• P2X7 alleles modulate LPS-stimulated cytokine production, and may serve as an amplification loop of innate immunity. (PMID:15120006)
• Arg(307) polymorphism abolishes the binding of ATP to the extracellular domain of P2X7. (PMID:15123679)
• Fibroblasts from type 2 diabetes patients are characterized by a hyperactive purinergic loop based either on a higher level of ATP release or on increased P2X7 reactivity. (PMID:15155383)
• the reversible permeabilization of erythrocytes by extracellular ATP is mediated by the P2X7 receptor (PMID:15304508)
• signaling via the P2X7R may modulate the astrocytic response to inflammation in the human central nervous system. (PMID:15472991)
• investigated P2X7 expression in 11 human hematopoietic cell lines, representing different lineages, as well as bone marrow mononuclear cells (BMMC) samples from 87 leukemia and 10 myelodysplastic syndrome (MDS) patients (PMID:15475073)
• P2X7/Ca2+ influx is modulated by estrogen in human ectocervical epithelial cells (PMID:15571247)
• A mechanism for P2X(7) receptor action, where activation involves a GRK-3-, beta-arrestin-2-, and dynamin-dependent internalization of the receptor into clathrin domains, followed in part by receptor degradation and recycling into the plasma membrane. (PMID:15728711)
• the P2X(7) receptor, via regulation of mature IL-1beta production, plays a common upstream transductional role in the development of pain of neuropathic and inflammatory origin. (PMID:15777864)
• the ability of P2X(7) polymorphisms to regulate the LPS-induced TNF-alpha to IL-10 ratio (PMID:15778408)
• Inflammatory stimuli drive P2X7 expression. The P2X7 receptor may play a role in the inflammatory responses against bacteria infection. (PMID:15830104)
• A 5’ intronic splice site polymorphism leads to a null allele of P2X7. (PMID:15862308)
• We report the identification of seven variants of human P2X7 which result from alternative splicing. (PMID:15896293)
• Current mapping suggests that murine P2RX7 receptor gene lies within lupus susceptibility locus SLEB4; P2RX7 receptor gene encodes a product with functional characteristics consistent with a role in systemic lupus erythematosus. (PMID:15899033)
• activation of the P2X7 ATP receptor elevates mitochondrial calcium and potential, increases cellular ATP levels, and promotes serum-independent growth (PMID:15901833)
• novel regulation of P2X7R outward and inward permeability to large molecules by Cl-(o) and Na+(o), respectively (PMID:15923180)
• The effect of polymorphisms in the P2X7 gene on the capacity of macrophages to kill mycobacteria is reported. (PMID:15942904)
• increased ATP-dependent activation of the P2X(7) 489T mutant with respect to the wild type receptor (PMID:15972634)
• findings have shown, for the first time, that functional P2X7 receptors are present in human melanomas and that their activation causes a decrease in cell number by apoptosis (PMID:15991050)
• Human Langerhans cells express functional P2X7 receptors, which play a role in the skin immune system. (PMID:16117789)
• P2X7 has a role in preventing apoptosis of human primary osteoclasts (PMID:16228288)
• P2X7 with a Thr357 to Ser polymorphism has absent or reduced function and impaired ATP-induced mycobacterial killing by macrophages (PMID:16263709)
• neuroblastoma cells seem to have molded P2X(7) function to their advantage in two ways (i.e., by silencing P2X(7) proapoptotic activity and by coupling P2X(7) stimulation to release of locally acting trophic factors) (PMID:16424024)
• a novel role for P2X(7) as a pro-inflammatory receptor involved in rapid MMP-9 release and leukocyte recruitment. (PMID:16514055)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	p2rx7	ENSDARG00000042440
mus_musculus	P2rx7	ENSMUSG00000029468
rattus_norvegicus	P2rx7	ENSRNOG00000001296

Paralogs (6): P2RX5 (ENSG00000083454), P2RX6 (ENSG00000099957), P2RX1 (ENSG00000108405), P2RX3 (ENSG00000109991), P2RX4 (ENSG00000135124), P2RX2 (ENSG00000187848)

Protein

Protein identifiers

P2X purinoceptor 7 — Q99572 (reviewed: Q99572)

Alternative names: ATP receptor, P2Z receptor, Purinergic receptor

All UniProt accessions (6): Q99572, A0A7G3W907, F5H237, F5H2X6, F5H8E7, J3KN30

UniProt curated annotations — full annotation on UniProt →

Function. ATP-gated nonselective transmembrane cation channel that requires high millimolar concentrations of ATP for activation. Upon ATP binding, it rapidly opens to allow the influx of small cations Na(+) and Ca(2+), and the K(+) efflux. Also has the ability to form a large pore in the cell membrane, allowing the passage of large cationic molecules. In microglia, may mediate NADPH transport across the plasma membrane. In immune cells, P2RX7 acts as a molecular sensor in pathological inflammatory states by detecting and responding to high local concentrations of extracellar ATP. In microglial cells, P2RX7 activation leads to the release of pro-inflammatory cytokines, such as IL-1beta and IL-18, through the activation of the NLRP3 inflammasome and caspase-1. Cooperates with KCNK6 to activate NLRP3 inflammasome. Activates death pathways leading to apoptosis and autophagy. Activates death pathways leading to pyroptosis. Shows ion channel activity but no macropore function. Non-functional channel. Non-functional channel.

Subunit / interactions. Homotrimers. Interacts with LAMA3, ITGB2, ACTB, ACTN4, SVIL, MPP3, HSPA1, HSPCB, HSPA8, PIK230 and PTPRB. Interacts (via C-terminus) with EMP2. Interacts with isoform B; this interaction potentiates P2RX7 responses.

Subcellular location. Cell membrane.

Tissue specificity. Widely expressed with highest levels in brain and immune tissues. Predominant form in many tissues.

Post-translational modifications. Phosphorylation results in its inactivation. ADP-ribosylation at Arg-125 is necessary and sufficient to activate P2RX7 and gate the channel. Palmitoylation of several cysteines in the C-terminal cytoplasmic tail is required for efficient localization to cell surface. Palmitoylation prevents channel desensitization by physically anchoring the palmitoylated groups to the membrane.

Activity regulation. Activated by high extracellular ATP levels (0.1-2.5 mM). The synthetic analog 2’(3’)-O-(4-benzoylbenzoyl)ATP (BzATP) acts as a potent agonist. Does not undergo desensitization, instead, undergoes a facilitation process where currents progressively increase with repetitive or prolonged agonist application. Palmitoylation prevents channel desensitization. The permeability of the P2RX7 channel is modulated by the amount of cholesterol in the plasma membrane.

Domain organisation. Contains two P2RX7-specific cytoplasmic domains, the C-cysteines (C-cys) anchor and the cytoplasmic ballast. Palmitoylation of the cytoplasmic C-cys anchor prevents receptor desensitization. The cytoplasmic ballast contains a zinc ion complex and a guanosine nucleotide binding site. The ion selectivity is determined by two sequential filters: a dynamic tri-Ser-342 size filter and three conformationally static cation filters.

Similarity. Belongs to the P2X receptor family.

Isoforms (9)

UniProt ID	Names	Canonical?
Q99572-1	A	yes
Q99572-2	B, Delta-C, cytoplasmic tail deleted
Q99572-3	C
Q99572-4	D
Q99572-5	E
Q99572-6	F
Q99572-7	G
Q99572-8	H, Delta-TM1
Q99572-9	J, Isoform P

RefSeq proteins (1): NP_002553* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001429	P2X_purnocptor	Family
IPR003050	P2X7_purinoceptor	Family
IPR027309	P2X_extracellular_dom_sf	Homologous_superfamily
IPR046815	P2RX7_C	Domain
IPR053792	P2X_RECEPTOR_CS	Conserved_site
IPR059116	P2X_receptor	Family

Pfam: PF00864, PF20478

Catalyzed reactions (Rhea), 3 shown:

• K(+)(in) = K(+)(out) (RHEA:29463)
• Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
• Na(+)(in) = Na(+)(out) (RHEA:34963)

UniProt features (91 total): sequence variant 28, binding site 15, splice variant 12, lipid moiety-binding region 5, glycosylation site 5, disulfide bond 5, site 4, modified residue 4, mutagenesis site 4, topological domain 3, transmembrane region 2, region of interest 2, chain 1, sequence conflict 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
9E3M	ELECTRON MICROSCOPY	2.48
9E3P	ELECTRON MICROSCOPY	2.53
9E3O	ELECTRON MICROSCOPY	2.76
9E3N	ELECTRON MICROSCOPY	2.95

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q99572-F1	88.27	0.65

Functional residue map

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

Catalytic / active sites (4): 14 (selectivity filter 2); 342 (selectivity filter 1); 352 (selectivity filter 2); 356 (selectivity filter 2)

Ligand- & substrate-binding residues (15): 311; 342; 479; 499; 506; 546; 547; 550; 567; 572; 583; 589 …

Post-translational modifications (9): 125, 133, 343, 390, 4, 362, 363, 374, 377

Disulfide bonds (5): 119–168, 129–152, 135–162, 216–226, 260–269

Glycosylation sites (5): 187, 202, 213, 241, 284

Mutagenesis-validated functional residues (4):

Position	Phenotype
14	loss of cation selectivity in favor of anion (cl(-)) selectivity; when associated with k-342 and k-352.
187	alters cell surface expression.
342	decreases the selectivity for na(+) over the larger organic cation tris(+). loss of cation selectivity in favor of anion
352	loss of cation selectivity in favor of anion (cl(-)) selectivity; when associated with k-14 and k-352.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-139853	Elevation of cytosolic Ca2+ levels
R-HSA-418346	Platelet homeostasis
R-HSA-844456	The NLRP3 inflammasome
R-HSA-9660826	Purinergic signaling in leishmaniasis infection
R-HSA-9856532	Mechanical load activates signaling by PIEZO1 and integrins in osteocytes

MSigDB gene sets: 597 (showing top): GOBP_POTASSIUM_ION_TRANSPORT, TAKEDA_TARGETS_OF_NUP98_HOXA9_FUSION_6HR_DN, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_POSITIVE_REGULATION_OF_LYMPHOCYTE_APOPTOTIC_PROCESS, GOBP_GLUTAMATE_SECRETION, GOBP_NUCLEOSIDE_DIPHOSPHATE_METABOLIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_ACID_SECRETION, GOBP_POSITIVE_REGULATION_OF_ADAPTIVE_IMMUNE_RESPONSE, GOBP_REGULATION_OF_ICOSANOID_SECRETION, GOBP_RESPONSE_TO_ZINC_ION, GOBP_RESPONSE_TO_ELECTRICAL_STIMULUS, GOBP_VACUOLE_ORGANIZATION

GO Biological Process (98): MAPK cascade (GO:0000165), cell morphogenesis (GO:0000902), phagolysosome assembly (GO:0001845), T cell mediated cytotoxicity (GO:0001913), positive regulation of T cell mediated cytotoxicity (GO:0001916), regulation of sodium ion transport (GO:0002028), response to ischemia (GO:0002931), membrane protein ectodomain proteolysis (GO:0006509), phospholipid transfer to membrane (GO:0006649), vesicle budding from membrane (GO:0006900), inflammatory response (GO:0006954), mitochondrion organization (GO:0007005), cell surface receptor signaling pathway (GO:0007166), protein secretion (GO:0009306), response to xenobiotic stimulus (GO:0009410), response to mechanical stimulus (GO:0009612), response to zinc ion (GO:0010043), positive regulation of calcium ion transport into cytosol (GO:0010524), positive regulation of gene expression (GO:0010628), glutamate secretion (GO:0014047), positive regulation of glutamate secretion (GO:0014049), gamma-aminobutyric acid secretion (GO:0014051), positive regulation of gamma-aminobutyric acid secretion (GO:0014054), synaptic vesicle exocytosis (GO:0016079), protein processing (GO:0016485), plasma membrane phospholipid scrambling (GO:0017121), sensory perception of pain (GO:0019233), calcium-mediated signaling (GO:0019722), protein catabolic process (GO:0030163), positive regulation of bone mineralization (GO:0030501), bleb assembly (GO:0032060), positive regulation of prostaglandin secretion (GO:0032308), prostaglandin secretion (GO:0032310), response to lipopolysaccharide (GO:0032496), positive regulation of interleukin-1 alpha production (GO:0032730), positive regulation of interleukin-1 beta production (GO:0032731), positive regulation of interleukin-6 production (GO:0032755), collagen metabolic process (GO:0032963), response to ATP (GO:0033198), response to fluid shear stress (GO:0034405)

GO Molecular Function (15): lipopolysaccharide binding (GO:0001530), purinergic nucleotide receptor activity (GO:0001614), extracellularly ATP-gated monoatomic cation channel activity (GO:0004931), signaling receptor binding (GO:0005102), potassium channel activity (GO:0005267), sodium channel activity (GO:0005272), ATP binding (GO:0005524), GTP binding (GO:0005525), identical protein binding (GO:0042802), metal ion binding (GO:0046872), nucleotide binding (GO:0000166), monoatomic ion channel activity (GO:0005216), protein binding (GO:0005515), channel activity (GO:0015267), signaling receptor activity (GO:0038023)

GO Cellular Component (13): cytoplasm (GO:0005737), mitochondrion (GO:0005739), plasma membrane (GO:0005886), cell-cell junction (GO:0005911), external side of plasma membrane (GO:0009897), membrane (GO:0016020), neuromuscular junction (GO:0031594), bleb (GO:0032059), neuronal cell body (GO:0043025), presynapse (GO:0098793), postsynapse (GO:0098794), endomembrane system (GO:0012505), synapse (GO:0045202)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Platelet calcium homeostasis	1
Hemostasis	1
Inflammasomes	1
Cell recruitment (pro-inflammatory response)	1
Cellular responses to mechanical stimuli	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	5
synapse	3
vesicle organization	2
membrane organization	2
secretion by cell	2
protein binding	2
monoatomic cation channel activity	2
purine ribonucleoside triphosphate binding	2
plasma membrane	2
intracellular signaling cassette	1
anatomical structure morphogenesis	1
phagocytosis	1
lysosome organization	1
organelle assembly	1
phagosome maturation	1
leukocyte mediated cytotoxicity	1
T cell mediated immunity	1
positive regulation of leukocyte mediated cytotoxicity	1
T cell mediated cytotoxicity	1
regulation of T cell mediated cytotoxicity	1
positive regulation of T cell mediated immunity	1
sodium ion transport	1
regulation of metal ion transport	1
response to stress	1
membrane protein proteolysis	1
phospholipid transport	1
vesicle-mediated transport	1
defense response	1
organelle organization	1
signal transduction	1
protein transport	1
establishment of protein localization to extracellular region	1
protein localization to extracellular region	1
response to chemical	1
response to external stimulus	1
response to abiotic stimulus	1
response to metal ion	1
positive regulation of cytosolic calcium ion concentration	1
regulation of calcium ion transport into cytosol	1
calcium ion transport into cytosol	1

Protein interactions and networks

STRING

1326 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
P2RX7	PANX1	Q96RD7	986
P2RX7	P2RX4	Q99571	946
P2RX7	P2RX1	P51575	872
P2RX7	NLRP3	Q96P20	863
P2RX7	CAMP	P49913	855
P2RX7	P2RX3	P56373	798
P2RX7	CASP1	P29466	784
P2RX7	P2RY2	P41231	768
P2RX7	P2RY12	Q9H244	724
P2RX7	P2RY1	P47900	721
P2RX7	TLR4	O00206	720
P2RX7	P2RY6	Q15077	705
P2RX7	ARL11	Q969Q4	697
P2RX7	MEFV	O15553	691
P2RX7	P2RY4	P51582	689

IntAct

41 interactions, top by confidence:

A	B	Type	Score
P2RX7	KRT31	psi-mi:“MI:0915”(physical association)	0.720
KRT31	P2RX7	psi-mi:“MI:0915”(physical association)	0.720
KRTAP10-8	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
P2RX7	KRTAP10-8	psi-mi:“MI:0915”(physical association)	0.560
TRIM27	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
HSF2BP	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
NOTCH2NLC	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
EFEMP2	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
CYSRT1	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
P2RX7	PLEKHF2	psi-mi:“MI:0915”(physical association)	0.560
KRT34	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
ZNF655	P2RX7	psi-mi:“MI:0915”(physical association)	0.560
ABL1	P2RX7	psi-mi:“MI:0915”(physical association)	0.400
GRB2	P2RX7	psi-mi:“MI:0915”(physical association)	0.400
P2RX7	NCK1	psi-mi:“MI:0915”(physical association)	0.400
EFNB3	P2RX7	psi-mi:“MI:0915”(physical association)	0.370
P2RX7	CASK	psi-mi:“MI:0915”(physical association)	0.370
P2RX7	TM9SF1	psi-mi:“MI:0915”(physical association)	0.370
EPHA1	P2RX7	psi-mi:“MI:0915”(physical association)	0.000
P2RX7	KRT31	psi-mi:“MI:0915”(physical association)	0.000
P2RX7	TRIM27	psi-mi:“MI:0915”(physical association)	0.000
P2RX7	HSF2BP	psi-mi:“MI:0915”(physical association)	0.000
P2RX7	NOTCH2NLC	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (20): P2RX7 (Two-hybrid), KRTAP10-8 (Two-hybrid), KRT31 (Two-hybrid), KRT34 (Two-hybrid), HSF2BP (Two-hybrid), EFEMP2 (Two-hybrid), PLEKHF2 (Two-hybrid), CYSRT1 (Two-hybrid), ZNF655 (Two-hybrid), TRIM27 (Two-hybrid), NOTCH2NL (Two-hybrid), NBPF19 (Two-hybrid), P2RX7 (Affinity Capture-MS), PXN (Affinity Capture-Western), P2RX7 (Affinity Capture-Western)

ESM2 similar proteins: A0ZSE6, A0ZT23, A4KX75, A5PLH4, A7MB71, F4IAL1, G0SDN0, O43173, P09534, P25656, P34389, P38566, P42838, P51578, P53740, P61644, P86091, Q09884, Q10351, Q17678, Q1MTQ5, Q25197, Q25410, Q2T9P5, Q3TT99, Q64663, Q64689, Q66KL4, Q6DE06, Q6ZXC8, Q7RTY8, Q86XS5, Q8BIK6, Q8IA41, Q8IA44, Q91VE2, Q94316, Q95JK4, Q96WW4, Q99572

Diamond homologs: F8W463, O15547, O54803, O70397, P47824, P49653, P49654, P51575, P51576, P51577, P51578, P51579, P56373, Q3UR32, Q5E9U1, Q64663, Q8K3P1, Q91VE2, Q93086, Q99571, Q99572, Q9JJX6, Q9UBL9, Q9Z1M0, Q86JM7

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
“GW 791343 HYDROCHLORIDE”	down-regulates	P2RX7	“chemical inhibition”
ATP	up-regulates	P2RX7	“chemical activation”
P2RX7	up-regulates	PLD2
clemastine	“up-regulates activity”	P2RX7	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	65
Likely benign	10
Benign	6

Top pathogenic / likely-pathogenic (0)

SpliceAI

1530 predictions. Top by Δscore:

Variant	Effect	Δscore
12:121133091:GTTTG:G	donor_gain	1.0000
12:121154783:A:AG	acceptor_gain	1.0000
12:121154784:G:GG	acceptor_gain	1.0000
12:121154784:GC:G	acceptor_gain	1.0000
12:121154784:GCTTT:G	acceptor_gain	1.0000
12:121154950:GCAG:G	donor_gain	1.0000
12:121154954:GTGA:G	donor_loss	1.0000
12:121154955:T:A	donor_loss	1.0000
12:121165352:CCCA:C	acceptor_loss	1.0000
12:121165353:CCA:C	acceptor_loss	1.0000
12:121165354:CA:C	acceptor_loss	1.0000
12:121165355:A:AG	acceptor_gain	1.0000
12:121165355:AG:A	acceptor_gain	1.0000
12:121165355:AGG:A	acceptor_loss	1.0000
12:121165356:G:A	acceptor_gain	1.0000
12:121165356:G:GT	acceptor_gain	1.0000
12:121165356:GGC:G	acceptor_gain	1.0000
12:121165356:GGCC:G	acceptor_gain	1.0000
12:121165356:GGCCT:G	acceptor_gain	1.0000
12:121165433:ACCAC:A	donor_gain	1.0000
12:121165434:CCAC:C	donor_gain	1.0000
12:121165434:CCACG:C	donor_loss	1.0000
12:121165435:CAC:C	donor_gain	1.0000
12:121165436:AC:A	donor_gain	1.0000
12:121165437:CGTA:C	donor_loss	1.0000
12:121165438:G:GG	donor_gain	1.0000
12:121165439:TAAG:T	donor_loss	1.0000
12:121166046:A:AG	acceptor_gain	1.0000
12:121167486:AG:A	acceptor_gain	1.0000
12:121167486:AGGGC:A	acceptor_gain	1.0000

AlphaMissense

3944 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:121175426:G:C	R307P	0.997
12:121162488:G:C	W167C	0.996
12:121162488:G:T	W167C	0.996
12:121160941:T:A	C135S	0.994
12:121160942:G:C	C135S	0.994
12:121162441:T:A	C152S	0.993
12:121162442:G:C	C152S	0.993
12:121162471:T:A	C162S	0.993
12:121162472:G:C	C162S	0.993
12:121167517:G:C	W258C	0.993
12:121167517:G:T	W258C	0.993
12:121162486:T:A	W167R	0.992
12:121162486:T:C	W167R	0.992
12:121162489:T:A	C168S	0.992
12:121162490:G:C	C168S	0.992
12:121162489:T:C	C168R	0.991
12:121160923:T:A	C129S	0.990
12:121160924:G:C	C129S	0.990
12:121165402:G:C	K193N	0.989
12:121165402:G:T	K193N	0.989
12:121167515:T:A	W258R	0.989
12:121167515:T:C	W258R	0.989
12:121167521:T:A	C260S	0.989
12:121167522:G:C	C260S	0.989
12:121165405:C:A	N194K	0.988
12:121165405:C:G	N194K	0.988
12:121162441:T:C	C152R	0.987
12:121162472:G:A	C162Y	0.987
12:121165395:T:C	L191P	0.986
12:121167523:C:G	C260W	0.986

dbSNP variants (sampled 300 via entrez): RS1000002654 (12:121168468 T>G), RS1000069620 (12:121135449 C>T), RS1000261111 (12:121153642 C>T), RS1000317086 (12:121175007 C>A), RS1000319471 (12:121152889 C>T), RS1000354182 (12:121141210 A>C,T), RS1000409341 (12:121180859 A>G), RS1000411278 (12:121147768 C>G,T), RS1000499877 (12:121164655 G>A,T), RS1000517340 (12:121160202 C>T), RS1000623422 (12:121154731 C>A,T), RS1000688538 (12:121186743 G>A), RS1000716479 (12:121164940 T>A,C), RS1000727026 (12:121159395 C>G,T), RS1000779552 (12:121159706 C>A)

Disease associations

OMIM: gene MIM:602566 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST001737_30	Chronic obstructive pulmonary disease-related biomarkers	4.000000e-06
GCST008362_48	Birth weight	1.000000e-08
GCST90011898_10	Alanine aminotransferase levels	6.000000e-12

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004811	interleukin-8 measurement
EFO:0004344	birth weight

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4524012 (PROTEIN FAMILY), CHEMBL4805 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

9 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 56,405 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL4173394	BRILLIANT BLUE G	4	14,477
CHEMBL265502	SURAMIN	3	36,848
CHEMBL13828	OXATOMIDE	2	4,199
CHEMBL1823817	CE-224535	2	126
CHEMBL3545108	AZD9056	2	137
CHEMBL3914857	ZANVIPIXANT	2	42
CHEMBL4079239	JNJ-54175446	2	62
CHEMBL1222883	GSK1482160	1	45
CHEMBL536151	IMD-0354	1	469

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1718125	Dosage	3	fentanyl	Pain;Postoperative

PharmGKB variants

6 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1718125	P2RX7	3	0.25	1	fentanyl
rs208293	P2RX7		0.00	0
rs1718136	P2RX7		0.00	0
rs7132846	P2RX7		0.00	0
rs2230912	P2RX7		0.00	0
rs1718119	P2RX7		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: lgic — P2X receptors

Most potent curated ligand interactions (16 total), top 16:

Ligand	Action	Affinity	Parameter
GSK1482160	Binding	8.94	pKd
JNJ-47965567	Antagonist	8.3	pIC50
A804598	Antagonist	8.0	pIC50
brilliant blue G	Antagonist	8.0	pIC50
A839977	Antagonist	7.7	pIC50
decavanadate	Antagonist	7.4	pA2
A740003	Antagonist	7.4	pIC50
A438079	Antagonist	6.9	pIC50
compound 16i [PMID: 31525963]	Antagonist	6.64	pIC50
GSK1370319A	Antagonist	6.32	pIC50
AZ11657312 (salt free)	Antagonist	6.1	pA2
BzATP	Agonist	5.33	pEC50
chelerythrine	Negative	5.25	pIC50
ITH15004	Antagonist	5.05	pIC50
oxidised ATP	Irreversible inhibition	3.5	pIC50
ATP	Agonist	3.11	pEC50

Binding affinities (BindingDB)

1923 measured of 2013 human assays (2017 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL550030	IC50	0.0501 nM
CHEMBL560506	IC50	0.0794 nM
2-chloro-N-[3-[1-(trifluoromethyl)cyclopropyl]-2-[6-(trifluoromethyl)-3-pyridinyl]propyl]benzamide	IC50	0.09 nM	US-9102591: Benzamides
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-(1,3-thiazol-4-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.2 nM	US-10047092
CHEMBL551360	IC50	0.2 nM
2,3-dichloro-N-[[4,4-difluoro-1-(6-fluoro-3-pyridinyl)cyclohexyl]methyl]benzamide	IC50	0.28 nM	US-9102591: Benzamides
(6S)-7-[2-Chloro-3-(trifluoromethyl)benzyl]-6-ethyl-3-pyrazin-2-yl-6,7-dihydro[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one	IC50	0.3 nM	US-10047092
2,3-dichloro-N-[3-cyclopropyl-2-[6-(trifluoromethyl)-3-pyridinyl]propyl]benzamide	IC50	0.31 nM	US-9102591: Benzamides
2,3-dichloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-(4-fluorophenyl)ethyl]benzamide	IC50	0.33 nM	US-9415055: Cyclic amines
BDBM160086	IC50	0.4 nM	US-10047092
2-chloro-N-[(2S)-2-(4-chlorophenyl)-2-morpholin-4-ylethyl]-3-methylbenzamide	IC50	0.53 nM	US-9593105: Cyclic amines
2-chloro-N-[[4,4-difluoro-1-[6-(trifluoromethyl)-3-pyridinyl]cyclohexyl]methyl]-3-methylbenzamide	IC50	0.54 nM	US-9102591: Benzamides
2,3-dichloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-(4-methoxyphenyl)ethyl]benzamide	IC50	0.6 nM	US-9415055: Cyclic amines
2,3-dichloro-N-[2-(4-chlorophenyl)-2-morpholin-4-ylethyl]benzamide	IC50	0.6 nM	US-9415055: Cyclic amines
2,3-dichloro-N-[(2S)-2-(4-chlorophenyl)-2-morpholin-4-ylethyl]benzamide	IC50	0.62 nM	US-9593105: Cyclic amines
2-chloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-[6-(trifluoromethyl)-3-pyridinyl]ethyl]-6-fluorobenzamide	IC50	0.62 nM	US-9415055: Cyclic amines
2,3-dichloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide	IC50	0.65 nM	US-9415055: Cyclic amines
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.7 nM	US-9040534: [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-3-[4-(hydroxymethyl)-2-pyridinyl]-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.7 nM	US-10047092
6-(trifluoromethyl)picolinohydrazide	IC50	0.7 nM	US-10053463: Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
3-bromo-N-[[4,4-difluoro-1-[6-(trifluoromethyl)-3-pyridinyl]cyclohexyl]methyl]-2-methylbenzamide	IC50	0.71 nM	US-9102591: Benzamides
2,6-dichloro-N-[3-cyclopropyl-2-[6-(trifluoromethyl)-3-pyridinyl]propyl]benzamide	IC50	0.71 nM	US-9102591: Benzamides
2-chloro-N-[[4,4-difluoro-1-(6-fluoro-3-pyridinyl)cyclohexyl]methyl]-5-methylbenzamide	IC50	0.76 nM	US-9102591: Benzamides
2,3-dichloro-N-[2-(6-cyclopropyl-3-pyridinyl)-3-[1-(difluoromethyl)cyclopropyl]propyl]benzamide	IC50	0.76 nM	US-9102591: Benzamides
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-cyclopropyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.8 nM	US-10047092
2,6-dichloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide	IC50	0.82 nM	US-9102591: Benzamides
2-chloro-N-[[4,4-difluoro-1-(6-fluoro-3-pyridinyl)cyclohexyl]methyl]-5-methoxybenzamide	IC50	0.83 nM	US-9102591: Benzamides
2,3-dichloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide	IC50	0.86 nM	US-9102591: Benzamides
2,3-dichloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-(6-fluoro-3-pyridinyl)ethyl]benzamide	IC50	0.89 nM	US-9415055: Cyclic amines
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-3-(5-fluoro-2-pyridinyl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.9 nM	US-10047092
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-ethyl-3-pyrimidin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	0.9 nM	US-10047092
2,3-dichloro-N-[[4,4-difluoro-1-[2-(trifluoromethyl)pyrimidin-5-yl]cyclohexyl]methyl]benzamide	IC50	0.95 nM	US-9102591: Benzamides
2,3-dichloro-N-[[4,4-difluoro-1-(6-methoxy-3-pyridinyl)cyclohexyl]methyl]benzamide	IC50	0.96 nM	US-9102591: Benzamides
(6S)-7-[(2,3-dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1 nM	US-9040534: [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-(1H-pyrazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1 nM	US-10047092
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyridin-3-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1 nM	US-10047092
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-3-(5-fluoropyrimidin-2-yl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1 nM	US-10047092
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-cyclopropyl-3-pyrimidin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1 nM	US-10047092
2,3-dichloro-N-[4-methyl-2-(6-methyl-3-pyridinyl)pentyl]benzamide	IC50	1 nM	US-9102591: Benzamides
6-methylpicolinohydrazide	IC50	1 nM	US-10053463: Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
(2,3-dichlorophenyl)-[(6S)-1-(5-fluoropyrimidin-2-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	IC50	1 nM	US-9464084: P2X7 modulators
CHEMBL556680	IC50	1 nM
7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-cyclopropyl-3-(1H-pyrazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1.1 nM	US-10047092
2,3-dichloro-N-[2-(4-fluorophenyl)-2-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide	IC50	1.1 nM	US-9102591: Benzamides
[2-chloro-3-(trifluoromethyl)phenyl]-[(1S,8R)-5-(5-fluoropyrimidin-2-yl)-3,4,6,12-tetrazatricyclo[6.3.1.02,6]dodeca-2,4-dien-12-yl]methanone	IC50	1.1 nM	US-10053462: P2X7 modulators
[2-chloro-3-(trifluoromethyl)phenyl]-[(6S)-6-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	IC50	1.1 nM	US-9464084: P2X7 modulators
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-(5-methyl-1H-pyrazol-3-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1.2 nM	US-10047092
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-(1,3-thiazol-2-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	IC50	1.2 nM	US-10047092
2-chloro-N-[[4,4-difluoro-1-(6-fluoro-3-pyridinyl)cyclohexyl]methyl]-5-(trifluoromethyl)benzamide	IC50	1.2 nM	US-9102591: Benzamides
2,3-dichloro-N-[[4,4-difluoro-1-[6-(trifluoromethyl)-3-pyridinyl]cyclohexyl]methyl]benzamide	IC50	1.2 nM	US-9102591: Benzamides

ChEMBL bioactivities

6100 potent at pChembl≥5 of 6100 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	IC50	0.01	nM	CHEMBL2324343
10.30	IC50	0.05012	nM	CHEMBL550030
10.22	IC50	0.06	nM	CHEMBL3415305
10.10	IC50	0.07943	nM	CHEMBL560506
10.05	IC50	0.09	nM	CHEMBL3679059
9.96	IC50	0.11	nM	CHEMBL4165149
9.82	IC50	0.15	nM	CHEMBL5430904
9.70	IC50	0.2	nM	CHEMBL3663257
9.70	IC50	0.2	nM	CHEMBL3663243
9.70	IC50	0.1995	nM	CHEMBL551360
9.64	IC50	0.23	nM	CHEMBL3415305
9.60	IC50	0.25	nM	CHEMBL6102198
9.55	IC50	0.28	nM	CHEMBL3679011
9.52	IC50	0.3	nM	CHEMBL3663294
9.52	IC50	0.3	nM	CHEMBL5923358
9.51	IC50	0.31	nM	CHEMBL3679036
9.50	IC50	0.3162	nM	CHEMBL564882
9.49	IC50	0.32	nM	CHEMBL4521847
9.48	IC50	0.33	nM	CHEMBL3984958
9.40	IC50	0.4	nM	CHEMBL3663316
9.40	IC50	0.3981	nM	CHEMBL551362
9.31	IC50	0.49	nM	CHEMBL4582650
9.30	IC50	0.5	nM	CHEMBL3663316
9.30	IC50	0.5	nM	CHEMBL3663244
9.30	IC50	0.5	nM	CHEMBL1824026
9.28	IC50	0.53	nM	CHEMBL3955749
9.27	IC50	0.54	nM	CHEMBL3679043
9.26	IC50	0.55	nM	CHEMBL3679036
9.22	IC50	0.6	nM	CHEMBL3663253
9.22	IC50	0.6	nM	CHEMBL3913134
9.22	IC50	0.6	nM	CHEMBL3916032
9.21	IC50	0.62	nM	CHEMBL4109892
9.21	IC50	0.62	nM	CHEMBL3958103
9.20	IC50	0.631	nM	CHEMBL1271548
9.19	IC50	0.65	nM	CHEMBL3913344
9.15	IC50	0.7	nM	CHEMBL3663242
9.15	IC50	0.7	nM	CHEMBL3663260
9.15	IC50	0.7	nM	CHEMBL3663255
9.15	IC50	0.71	nM	CHEMBL3679042
9.15	IC50	0.71	nM	CHEMBL3679084
9.15	IC50	0.7	nM	CHEMBL5749245
9.12	IC50	0.76	nM	CHEMBL3639778
9.12	IC50	0.76	nM	CHEMBL3679051
9.12	IC50	0.76	nM	CE-224535
9.10	IC50	0.7943	nM	CHEMBL2218174
9.10	IC50	0.7943	nM	CHEMBL2218383
9.10	IC50	0.7943	nM	CHEMBL2218569
9.10	IC50	0.8	nM	CHEMBL3663286
9.10	IC50	0.79	nM	CHEMBL3679051
9.10	IC50	0.8	nM	CE-224535

PubChem BioAssay actives

1817 with measured affinity, of 3180 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[2-[(2R)-1-aminopropan-2-yl]-6-methyl-1-oxoisoquinolin-5-yl]-2-[3-fluoro-4-(trifluoromethyl)phenyl]acetamide	726095: Inhibition of P2X7 receptor (unknown origin) assessed as inhibition of IL1beta production	ic50	<0.0001	uM
N-(1-adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide;hydrochloride	1636667: Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA	ic50	0.0001	uM
[4-[3-[1-[4-(dimethylamino)benzoyl]piperidin-4-yl]imidazol-4-yl]phenyl] isoquinoline-5-sulfonate	1358119: Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake	ic50	0.0001	uM
2-(1-adamantyl)-N-[2-(1-hydroxy-3-methylbutan-2-yl)-1-oxoisoquinolin-5-yl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0001	uM
2-(1-adamantyl)-N-[2-[(2S)-1-hydroxypropan-2-yl]-1-oxoisoquinolin-5-yl]acetamide	2008042: Inhibition of P2X7 (unknown origin) assessed as reduction in IL-1 beta release	ic50	0.0001	uM
(2S)-2-[5-[[2-(1-adamantyl)acetyl]amino]-6-chloro-1-oxoisoquinolin-2-yl]propanamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0001	uM
2-(1-adamantyl)-N-[2-(1,3-dihydroxypropan-2-yl)-1-oxoisoquinolin-5-yl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0002	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-3-(4-fluorophenyl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0002	uM
[4-[3-[1-(4-methylsulfonylbenzoyl)piperidin-4-yl]imidazol-4-yl]phenyl] isoquinoline-5-sulfonate	1636667: Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA	ic50	0.0003	uM
N-(6-chloro-2-cyclopropyl-1-oxoisoquinolin-5-yl)-2-[2-fluoro-3-(trifluoromethyl)phenyl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0003	uM
2,3-dichloro-N-[2-(4,4-difluoropiperidin-1-yl)-2-(4-fluorophenyl)ethyl]benzamide	1627294: Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium mobilization monitored for 5 mins followed by stimulation with BzATP measured after 3 mins by Fluo-8 NW dye based tetra FLIPR assay	ic50	0.0003	uM
2-[3-fluoro-4-(trifluoromethyl)phenyl]-N-[2-[(2R)-1-hydroxypropan-2-yl]-6-methyl-1-oxoisoquinolin-5-yl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0004	uM
[4-[3-[1-[4-(dimethylamino)benzoyl]piperidin-4-yl]imidazol-4-yl]phenyl] 3-(cyclopropylcarbamoyl)benzenesulfonate	1636666: Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluorescence analysis	ic50	0.0005	uM
5-[1-[(2S)-3-amino-2-hydroxypropyl]-5-methylpyrazol-3-yl]-2-chloro-N-[(1-hydroxycycloheptyl)methyl]benzamide;hydrochloride	616425: Antagonist activity at P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced YO-PRO-1 uptake	ic50	0.0005	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyridin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0005	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrimidin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0005	uM
(4S)-N-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-1,3-dimethyl-2-oxoimidazolidine-4-carboxamide	528215: Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells by ethidium accumulation assay	ic50	0.0006	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-(1H-pyrazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0006	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0007	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-3-(5-fluoro-2-pyridinyl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0007	uM
2-chloro-N-[(1-hydroxycycloheptyl)methyl]-5-[4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-1,2,4-triazin-2-yl]benzamide	1831762: Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis	ic50	0.0008	uM
2,3-dichloro-N-[2-(6-cyclopropyl-3-pyridinyl)-3-[1-(difluoromethyl)cyclopropyl]propyl]benzamide	1627294: Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium mobilization monitored for 5 mins followed by stimulation with BzATP measured after 3 mins by Fluo-8 NW dye based tetra FLIPR assay	ic50	0.0008	uM
[3-(18F)fluoro-2-(trifluoromethyl)-4-pyridinyl]-[(6S)-6-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	1896057: Inhibition of human P2X7R	ic50	0.0010	uM
tert-butyl 4-[2-(isoquinolin-5-ylsulfonylamino)-3-(4-isoquinolin-5-ylsulfonyloxyphenyl)propanoyl]piperazine-1-carboxylate	150180: Antagonistic activity against P2X7 receptor	ic50	0.0010	uM
2-(1-adamantyl)-N-[1-oxo-2-[[(2R)-pyrrolidin-2-yl]methyl]isoquinolin-5-yl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0010	uM
2-(1-adamantyl)-N-[2-[(2R)-1-hydroxypropan-2-yl]-1-oxoisoquinolin-5-yl]acetamide	2008042: Inhibition of P2X7 (unknown origin) assessed as reduction in IL-1 beta release	ic50	0.0010	uM
3-chloro-N’-quinolin-5-yladamantane-1-carbohydrazide	408591: Antagonist activity at human recombinant P2X7 receptor expressed in differentiated human THP1 cells assessed as inhibition of benzoyl-ATP-induced IL1-beta release by ELISA	ic50	0.0010	uM
(6S)-7-[(2,3-dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0010	uM
[2-chloro-3-(trifluoromethyl)phenyl]-[(1S,8R)-5-(5-fluoropyrimidin-2-yl)-3,4,6,12-tetrazatricyclo[6.3.1.02,6]dodeca-2,4-dien-12-yl]methanone	2008063: Inhibition of recombinant human P2X7 receptor by FLIPR assay	ic50	0.0011	uM
[4-[[6-[4-[4-(dimethylamino)benzoyl]piperazin-1-yl]-2,4-dioxopyrimidin-1-yl]methyl]phenyl] isoquinoline-5-sulfonate	1636667: Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA	ic50	0.0013	uM
2-[4-chloro-3-(trifluoromethyl)phenyl]-N-[2-[(2R)-1-hydroxypropan-2-yl]-1-oxoisoquinolin-5-yl]acetamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	ic50	0.0013	uM
4-bromo-N’-(3,5-dichloro-4-pyridinyl)adamantane-2-carbohydrazide	669103: Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA	ic50	0.0013	uM
N-[(2,4-dichloro-6-methylphenyl)methyl]-3,4-dihydro-2H-pyrano[2,3-b]pyridine-4-carboxamide	1627292: Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced calcium mobilization incubated for 90 mins in presence of ATP by YO-PRO-1 dye based tetra FLIPR assay	ic50	0.0013	uM
[2-chloro-3-(trifluoromethyl)phenyl]-[(6R)-6-methyl-1-pyridin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	2008065: Antagonist activity at recombinant human P2X7 receptor expressed in 1321N1 cells measured after 30 mins by fluorescence based calcium flux assay	ic50	0.0013	uM
[4-[(2S)-3-[4-(4-fluorophenyl)piperazin-1-yl]-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonate	1066085: Antagonist activity at P2X7 receptor (unknown origin)	ic50	0.0013	uM
(2,3-dichlorophenyl)-[(8R)-8-methyl-3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone	1239720: Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0014	uM
[4-[3-[1-(4-nitrobenzoyl)piperidin-4-yl]imidazol-4-yl]phenyl] isoquinoline-5-sulfonate	1636666: Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluorescence analysis	ic50	0.0015	uM
N-(2-adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide;hydrochloride	1358119: Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake	ic50	0.0015	uM
N-[(2,4-dichloro-6-methylphenyl)methyl]-5,6-dihydro-4H-cyclopenta[d][1,3]thiazole-6-carboxamide	1627292: Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced calcium mobilization incubated for 90 mins in presence of ATP by YO-PRO-1 dye based tetra FLIPR assay	ic50	0.0015	uM
N-(1-adamantylmethyl)-2-chloro-5-methoxybenzamide	423041: Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake	kd	0.0016	uM
(2S)-N-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-1-ethyl-5-oxopyrrolidine-2-carboxamide	501681: Inhibition of human P2X7 receptor by ethidium bromide release assay	ic50	0.0016	uM
N-(1-adamantylmethyl)-2,3-dichlorobenzamide	150181: Antagonistic activity against the P2X7 ion channel	kd	0.0016	uM
[2-chloro-3-(trifluoromethyl)phenyl]-[(6S)-6-methyl-1-pyridin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	1478240: Antagonist activity at human recombinant P2X7 expressed in 1321N1 cells assessed as inhibition of BzATP-induced calcium mobilization after 30 mins by calcium-4 staining based FLIPR assay	ic50	0.0017	uM
6-(3-chloro-2-methylanilino)-4-phenyl-3,4-dihydro-1H-pyrimido[6,1-c][1,4]oxazin-8-one	2008059: Antagonist activity at human P2X7 receptor	ic50	0.0018	uM
[4-[3-[1-[4-chloro-3-(trifluoromethyl)benzoyl]piperidin-4-yl]imidazol-4-yl]phenyl] 3-(methylcarbamoyl)benzenesulfonate	1636667: Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta release per-incubated for 30 mins before BzATP addition and measured after 30 mins by ELISA	ic50	0.0018	uM
[2-chloro-3-(trifluoromethyl)phenyl]-[(6S)-1-(1-ethylpyrazol-3-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	1478240: Antagonist activity at human recombinant P2X7 expressed in 1321N1 cells assessed as inhibition of BzATP-induced calcium mobilization after 30 mins by calcium-4 staining based FLIPR assay	ic50	0.0018	uM
(2S)-N-[[2-iodo-3-(trifluoromethyl)phenyl]methyl]-1-methyl-5-oxopyrrolidine-2-carboxamide	1543108: Competitive displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay	ki	0.0019	uM
(2,3-dichlorophenyl)-(3-pyrazin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanone	1239720: Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0019	uM
(6S)-7-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyridin-3-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-one	1269196: Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assay	ic50	0.0019	uM
[2-chloro-3-(trifluoromethyl)phenyl]-[(6S)-1-(5-fluoropyrimidin-2-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone	1478240: Antagonist activity at human recombinant P2X7 expressed in 1321N1 cells assessed as inhibition of BzATP-induced calcium mobilization after 30 mins by calcium-4 staining based FLIPR assay	ic50	0.0019	uM

CTD chemical–gene interactions

58 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Adenosine Triphosphate	decreases reaction, increases secretion, increases transport, increases response to substance, affects binding (+4 more)	6
3’-O-(4-benzoyl)benzoyladenosine 5’-triphosphate	increases import, increases phosphorylation, increases secretion, affects reaction, decreases reaction (+1 more)	5
KN 62	increases secretion, affects binding, decreases activity, decreases reaction, increases activity (+2 more)	3
Benzo(a)pyrene	increases methylation, affects methylation, decreases expression, increases expression	3
AZ10606120	decreases reaction, increases activity, decreases activity	2
coomassie Brilliant Blue	decreases reaction, increases activity, affects binding, decreases activity	2
sodium arsenite	increases expression, affects cotreatment, increases abundance	2
Air Pollutants, Occupational	affects expression, decreases expression	2
Arsenic	decreases expression, increases abundance, affects cotreatment, increases expression	2
Lipopolysaccharides	affects cotreatment, increases expression, decreases reaction	2
Toluene 2,4-Diisocyanate	affects response to substance, increases expression, increases reaction, increases secretion	2
Aflatoxin B1	decreases expression, increases methylation	2
GSK-J4	increases expression	1
FR900359	decreases phosphorylation	1
bisphenol F	increases activity	1
ZINC58368839	affects binding, decreases reaction, increases activity	1
ZINC09315614	decreases reaction, increases activity	1
TL8-506	increases expression, affects cotreatment	1
triphenyl phosphate	affects expression	1
bisphenol A	increases activity	1
protoberberine	decreases reaction, increases activity, increases import, increases phosphorylation, increases secretion	1
sodium arsenate	decreases expression, increases abundance	1
perfluorooctanoic acid	increases expression	1
tris(chloroethyl)phosphate	increases expression	1
calmidazolium	affects binding, decreases reaction, increases activity	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, increases expression, decreases reaction	1
avobenzone	decreases expression	1
tri-(2-chloroisopropyl)phosphate	increases expression	1
pyridoxal phosphate-6-azophenyl-2’,4’-disulfonic acid	affects binding, decreases reaction, increases activity	1
perfluoro-n-nonanoic acid	increases expression	1

ChEMBL screening assays

368 unique, capped per target: 293 binding, 75 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4339641	Binding	Negative allosteric modulation of human P2X expressed in Xenopus laevis oocytes assessed as inhibition of ATP-induced current response at 30 uM at -40 mV holding potential by two-electrode voltage clamp method relative to ATP alone	Di-aryl Sulfonamide Motif Adds π-Stacking Bulk in Negative Allosteric Modulators of the NMDA Receptor. — ACS Med Chem Lett
CHEMBL1017981	Functional	Antagonist activity at P2X7 receptor up to 10 uM	Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. — Bioorg Med Chem Lett

Cellosaurus cell lines

4 cell lines: 3 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0YM	B’SYS HEK 293 P2X7	Transformed cell line	Female
CVCL_D1Y0	Abcam A-549 P2RX7 KO	Cancer cell line	Male
CVCL_D2C9	Abcam HCT 116 P2RX7 KO	Cancer cell line	Male
CVCL_D2NS	Abcam THP-1 P2RX7 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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