P2RY2

Summary

P2RY2 (purinergic receptor P2Y2, HGNC:8541) is a protein-coding gene on chromosome 11q13.4, encoding P2Y purinoceptor 2 (P41231). Receptor for ATP and UTP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system.

The product of this gene belongs to the family of P2 receptors, which is activated by extracellular nucleotides and subdivided into P2X ligand-gated ion channels and P2Y G-protein coupled receptors. This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor, found on many cell types, is activated by ATP and UTP and is reported to be overexpressed on some cancer cell types. It is involved in many cellular functions, such as proliferation, apoptosis and inflammation. Three transcript variants encoding the same protein have been identified for this gene.

Source: NCBI Gene 5029 — RefSeq curated summary.

At a glance

• GWAS associations: 19
• Clinical variants (ClinVar): 80 total
• Druggable target: yes — 8 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002564

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8541
Approved symbol	P2RY2
Name	purinergic receptor P2Y2
Location	11q13.4
Locus type	gene with protein product
Status	Approved
Aliases	P2U
Ensembl gene	ENSG00000175591
Ensembl biotype	protein_coding
OMIM	600041
Entrez	5029

Gene structure

Transcript identifiers

Ensembl transcripts: 29 — 29 protein_coding

ENST00000311131, ENST00000393596, ENST00000393597, ENST00000892905, ENST00000892906, ENST00000892907, ENST00000892908, ENST00000892909, ENST00000892910, ENST00000892911, ENST00000892912, ENST00000892913, ENST00000892914, ENST00000892915, ENST00000968523, ENST00000968524, ENST00000968525, ENST00000968526, ENST00000968527, ENST00000968528, ENST00000968529, ENST00000968530, ENST00000968531, ENST00000968532, ENST00000968533, ENST00000968534, ENST00000968535, ENST00000968536, ENST00000968537

RefSeq mRNA: 3 — MANE Select: NM_002564 NM_002564, NM_176071, NM_176072

CCDS: CCDS8219

Canonical transcript exons

ENST00000393597 — 3 exons

Exon	Start	End
ENSE00001325561	73227981	73228175
ENSE00002213768	73218281	73218432
ENSE00002276368	73234156	73242427

Expression profiles

Bgee: expression breadth ubiquitous, 187 present calls, max score 91.53.

FANTOM5 (CAGE): breadth broad, TPM avg 2.9819 / max 202.8654, expressed in 625 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
115771	1.1588	434
115774	0.8264	315
115772	0.4740	232
115773	0.4304	214
115769	0.0607	27
115768	0.0315	11

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
hindlimb stylopod muscle	UBERON:0004252	91.53	gold quality
gastrocnemius	UBERON:0001388	91.06	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	90.10	gold quality
muscle of leg	UBERON:0001383	89.49	gold quality
muscle organ	UBERON:0001630	88.25	gold quality
esophagus mucosa	UBERON:0002469	86.86	gold quality
skeletal muscle tissue	UBERON:0001134	85.48	gold quality
vastus lateralis	UBERON:0001379	84.98	silver quality
biceps brachii	UBERON:0001507	84.65	gold quality
quadriceps femoris	UBERON:0001377	84.62	silver quality
esophagus squamous epithelium	UBERON:0006920	83.37	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	83.20	gold quality
epithelium of esophagus	UBERON:0001976	83.17	gold quality
lower esophagus mucosa	UBERON:0035834	81.80	gold quality
deltoid	UBERON:0001476	81.51	silver quality
gingival epithelium	UBERON:0001949	81.22	gold quality
squamous epithelium	UBERON:0006914	80.76	gold quality
triceps brachii	UBERON:0001509	80.58	gold quality
gingiva	UBERON:0001828	80.41	gold quality
muscle tissue	UBERON:0002385	80.36	gold quality
monocyte	CL:0000576	80.05	gold quality
gluteal muscle	UBERON:0002000	79.66	gold quality
mononuclear cell	CL:0000842	79.50	gold quality
body of tongue	UBERON:0011876	79.43	silver quality
leukocyte	CL:0000738	79.05	gold quality
heart left ventricle	UBERON:0002084	78.99	gold quality
endometrium epithelium	UBERON:0004811	78.90	silver quality
palpebral conjunctiva	UBERON:0001812	78.80	gold quality
apex of heart	UBERON:0002098	78.65	gold quality
cardiac ventricle	UBERON:0002082	78.53	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	2.49

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): RELA

miRNA regulators (miRDB)

273 targeting P2RY2, 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-8485	100.00	77.57	4731
HSA-MIR-4481	100.00	66.42	1669
HSA-MIR-4673	100.00	66.64	1490
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-4692	100.00	67.32	2066
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-10401-5P	99.99	65.79	948
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-4514	99.99	67.10	1870
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-23B-5P	99.98	66.07	587
HSA-MIR-4645-5P	99.98	65.81	1284
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-1229-3P	99.97	66.49	906
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-4487	99.96	64.58	1252
HSA-MIR-23A-5P	99.94	65.39	468
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-6753-3P	99.93	66.57	637
HSA-MIR-7107-3P	99.93	66.73	627
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-345-3P	99.89	70.23	1421
HSA-MIR-6780A-5P	99.88	66.69	2776
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-3941	99.86	70.54	2735
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-4447	99.85	67.81	2900

Literature-anchored findings (GeneRIF, showing 40)

• Ken is a novel regulator of JAK/STAT signaling whose dynamic spatial and temporal expression is capable of selectively modulating the transcriptional repertoire elicited by activated STAT92E in vivo. (PMID:16401426)
• Ken and barbie mutants have defects in escape behaviour, behavioural responses to visual stimuli and synaptic functions in the giant fibre system. (PMID:16879616)
• Data show that that BCL6 homolog ken and barbie (Ken) has an important role in the inhibition of somatic cyst stem cells (CySCs) differentiation. (PMID:22580161)
• In ken/barbie male flies lacking external genitalia, courtship and physical contact without ejaculation was unable to replicate the mating effect. (PMID:28851647)
• expression profile in human peripheral tissues and brain regions using PCR (PMID:11690642)
• Human keratinocytes express multiple P2Y-receptors: evidence for functional P2Y1, P2Y2, and P2Y4 receptors. (PMID:12603858)
• Adenine and uracil nucleotides differentially activate this receptor, which regulates the proliferation of lung cancer cells (PMID:12691958)
• a novel role for the P2Y2 receptor in expression of VCAM-1 that mediates the recruitment of monocytes by vascular endothelium associated with the development of atherosclerosis (PMID:12714597)
• 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)
• Non-melanoma skin cancers express functional purinergic receptors and that P2X7 receptor agonists significantly reduce cell numbers in vitro. (PMID:12880424)
• Fibrinogen is required for nucleotide-induced primary granule release from human neutrophils through the P2Y2 receptor without a role for arachidonic acid metabolites. (PMID:14613890)
• ADP-mediated P2Y1 and P2Y12 receptor activation supports LPA-induced platelet aggregation. (PMID:14645014)
• data suggest that agonist-induced binding of Src kinase to the Src homology 3 binding sites in the P2Y(2) purinergic receptor facilitates Src activation and allows Src to efficiently phosphorylate the epidermal growth factor receptor (PMID:14670955)
• activation of the P2Y(2)R induced rapid tyrosine phosphorylation of vascular endothelial growth factor receptor (VEGFR)-2 in human coronary artery endothelial cells (PMID:15175347)
• The P2Y2 is localized on trophoblastic villi. (PMID:15590415)
• activation of the G protein-coupled P2Y2 receptor (P2Y2R) subtype expressed in human 1321N1 astrocytoma cells enhanced the release of sAPP alpha in a time- and dose-dependent manner (PMID:15778502)
• the P2Y2 receptor apical targeting signal is located in its first extracellular loop (PMID:15908695)
• the RGD-dependent interaction between the P2Y(2)R and alpha(v) integrins is necessary for the P2Y(2)R to activate G(o) and to initiate G(o)-mediated signaling events leading to chemotaxis (PMID:16186116)
• Our results indicate a role for receptor phosphorylation by phorbol-insensitive protein kinases in agonist-induced desensitization of the P2Y2 nucleotide receptor. (PMID:16311903)
• P2Y2 receptor gene haplotypes influence intracellular Ca2+-release (PMID:16495779)
• UTP is a cardiac inotropic factor most likely by activation of P2Y2 receptors in man. (PMID:16543499)
• These results suggest that P2Y receptor-mediated and gap junction-mediated mechanisms of intercellular calcium signaling may play different roles during differentiation of bone-forming cells. (PMID:16545868)
• Stimulation of ARO cells evidenced a major involvement of P2Y1 and P2Y2 receptors in controlling the Hsp90 activation. P2Y1 and P2Y2 resulted significantly upregulated in sample biopsies from different thyroid tumors. (PMID:16741950)
• ATP release and autocrine feedback through P2Y2 and A3 receptors provide signal amplification, controlling gradient sensing and migration of neutrophils (PMID:17170310)
• P2Y(2) nucleotide receptors in U937 monocytic cells regulate the activation of extracellular signal-regulated kinases 1 and 2 (ERK 1/2) by inducing the clustering of alpha(v) integrins. (PMID:17186500)
• Alpha v integrin complexes provide the P2Y2R with access to G alpha12 protein, thereby allowing activation of this heterotrimeric G protein that controls actin cytoskeletal rearrangements required for chemotaxis. (PMID:17452627)
• These results suggest that P2Y2R activation in salivary gland cells increases the EGFR-dependent expression of VCAM-1 and the binding of lymphocytes. (PMID:17599409)
• Activation inhibits keratinocyte cell spreading and induces lamellipodium withdrawal. (PMID:17609252)
• ATP activated MAPKs through the P2Y2 purinoceptor/PLC/PKC/ERK signaling pathway and induced translocation of ERK1/2 into the nucleus. (PMID:18434089)
• functional P(2Y2) receptors in human valvular myofibroblasts are responsible for the Ca(2+) signals. (PMID:18475022)
• These results provide a basis for considering P2Y2 receptor changes as a neurochemical substrate of Alzheimer’s disease (PMID:18506388)
• P2UR desensitization on single endothelial cells is reported. (PMID:18568944)
• Expression and localization of the nucleotide selective P(2Y2) and P(2X1) receptors suggest that these receptors may mediate ATP-induced vasodilation in skeletal muscle. (PMID:19118095)
• Nucleotide mediated activation of the epithelial P2Y2 receptor promotes the transepithelial migration and adhesion of macrophages to the apical surface of intestinal epithelial cells. (PMID:19634190)
• The rs4944831 and the T-A-G haplotype of the human P2RY2 gene might be genetic markers for essential hypertension in Japanese men. (PMID:19710694)
• Upregulation and activation of the P2Y2 receptor stimulates cyclooxygenase-2 expression and prostaglandin E2 secretion by intestinal epithelial cells under proinflammatory conditions. (PMID:19734210)
• Extracellular nucleotides, via P2Y2 and P2Y6 receptors, regulate neutrophil migration by controlling TLR2-induced IL-8 release from human monocytes. (PMID:19735076)
• T-A-G haplotype of the human P2RY2 gene is a susceptibility haplotype for cerebral infarction in Japanese subjects (PMID:19763137)
• Genotype/haplotypes of human P2RY2 could be genetic markers for myocardial infarction in Japanese men. (PMID:19797825)
• Expression is reduced in typ3 2 diabetes, not due to alterations in receptor distribution and mRNA expression, but may be due to differences in receptor sensitivity. (PMID:19808895)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	p2ry2.1	ENSDARG00000099915
danio_rerio	p2ry2.3	ENSDARG00000104425
danio_rerio	p2ry2.2	ENSDARG00000104927
mus_musculus	P2ry2	ENSMUSG00000032860
rattus_norvegicus	P2ry2	ENSRNOG00000019283

Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR2 (ENSG00000126262), FFAR1 (ENSG00000126266), OXER1 (ENSG00000162881), OXGR1 (ENSG00000165621), P2RY1 (ENSG00000169860), P2RY6 (ENSG00000171631), GPR82 (ENSG00000171657), HCAR2 (ENSG00000182782), FFAR3 (ENSG00000185897), P2RY4 (ENSG00000186912), HCAR1 (ENSG00000196917), SUCNR1 (ENSG00000198829), HCAR3 (ENSG00000255398)

Protein

Protein identifiers

P2Y purinoceptor 2 — P41231 (reviewed: P41231)

Alternative names: ATP receptor, P2U purinoceptor 1, P2U receptor 1, Purinergic receptor

All UniProt accessions (1): P41231

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for ATP and UTP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system. The affinity range is UTP = ATP > ATP-gamma-S » 2-methylthio-ATP = ADP.

Subcellular location. Cell membrane.

Tissue specificity. Spleen, testis, kidney, liver, lung, heart and brain.

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

RefSeq proteins (3): NP_002555, NP_788085, NP_788086 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000356	P2Y2_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (26 total): topological domain 8, transmembrane region 7, sequence variant 3, glycosylation site 2, sequence conflict 2, chain 1, region of interest 1, compositionally biased region 1, disulfide bond 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
9K20	ELECTRON MICROSCOPY	2.65
9K0X	ELECTRON MICROSCOPY	2.83
9K25	ELECTRON MICROSCOPY	3.31

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P41231-F1	79.11	0.50

Antibody-complex structures (SAbDab): 3 — 9K0X, 9K20, 9K25

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 (1): 106–183

Glycosylation sites (2): 9, 13

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-416476	G alpha (q) signalling events
R-HSA-417957	P2Y receptors
R-HSA-5683826	Surfactant metabolism
R-HSA-9856530	High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells

MSigDB gene sets: 180 (showing top): GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, GOBP_CIRCULATORY_SYSTEM_PROCESS, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, REACTOME_P2Y_RECEPTORS, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, chr11q13, ONDER_CDH1_TARGETS_3_DN, GOBP_CELLULAR_RESPONSE_TO_ATP, GOBP_REGULATION_OF_ANATOMICAL_STRUCTURE_SIZE, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_SECRETION, GOBP_RESPONSE_TO_ATP

GO Biological Process (8): intracellular monoatomic ion homeostasis (GO:0006873), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589), positive regulation of mucus secretion (GO:0070257), cellular response to ATP (GO:0071318), blood vessel diameter maintenance (GO:0097746), signal transduction (GO:0007165)

GO Molecular Function (6): A1 adenosine receptor binding (GO:0031686), signaling receptor activity (GO:0038023), G protein-coupled purinergic nucleotide receptor activity (GO:0045028), G protein-coupled UTP receptor activity (GO:0045030), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

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

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
GPCR downstream signalling	1
Nucleotide-like (purinergic) receptors	1
Metabolism of proteins	1
Response of endothelial cells to shear stress	1

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
monoatomic ion homeostasis	1
intracellular chemical homeostasis	1
signal transduction	1
phospholipase C activator activity	1
purinergic nucleotide receptor signaling pathway	1
positive regulation of secretion	1
positive regulation of multicellular organismal process	1
mucus secretion	1
regulation of mucus secretion	1
response to ATP	1
cellular response to nitrogen compound	1
cellular response to oxygen-containing compound	1
vascular process in circulatory system	1
blood circulation	1
regulation of tube diameter	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
adenosine receptor binding	1
molecular transducer activity	1
purinergic nucleotide receptor activity	1
G protein-coupled purinergic nucleotide receptor signaling pathway	1
G protein-coupled pyrimidinergic nucleotide receptor activity	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

972 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
P2RY2	ENTPD1	P49961	935
P2RY2	P2RX1	P51575	928
P2RY2	GNAQ	P50148	860
P2RY2	P2RX4	Q99571	849
P2RY2	P2RX2	Q9UBL9	811
P2RY2	P2RX5	Q93086	804
P2RY2	P2RX3	P56373	788
P2RY2	P2RX6	O15547	768
P2RY2	P2RX7	Q99572	768
P2RY2	PANX1	Q96RD7	721
P2RY2	ENTPD8	Q5MY95	719
P2RY2	ENTPD3	O75355	713
P2RY2	SRC	P12931	712
P2RY2	ARRB1	P49407	676
P2RY2	FLNA	P21333	672

IntAct

6 interactions, top by confidence:

A	B	Type	Score
BRK1	P2RY2	psi-mi:“MI:0915”(physical association)	0.560
P2RY2	NHERF1	psi-mi:“MI:0407”(direct interaction)	0.440
P2RY2	SCAMP3	psi-mi:“MI:0914”(association)	0.350

BioGRID (107): P2RY2 (Affinity Capture-RNA), SRC (Affinity Capture-Western), CDH5 (Affinity Capture-Western), P2RY2 (Affinity Capture-RNA), NLRP3 (Affinity Capture-Western), NLRP3 (Co-localization), GOLGA5 (Affinity Capture-MS), SLC19A2 (Affinity Capture-MS), ERGIC3 (Affinity Capture-MS), APOB (Affinity Capture-MS), STX5 (Affinity Capture-MS), TPCN1 (Affinity Capture-MS), NUP205 (Affinity Capture-MS), RABL3 (Affinity Capture-MS), VKORC1L1 (Affinity Capture-MS)

ESM2 similar proteins: A7YY44, B2GV46, O14843, O15529, O15552, O35811, O46685, O88855, O93361, P34996, P35383, P41231, P41232, P46093, P47900, P48042, P49650, P49651, P49652, P50132, P51582, P55085, P55086, P58825, P58826, P59902, Q09QM4, Q13304, Q15077, Q15743, Q1JQB3, Q2HJA4, Q3UFD7, Q4KLH9, Q5YA25, Q63371, Q63645, Q6IYF8, Q6NS65, Q6Y1R5

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, A6QLE7, D4A7K7, E7FEL0, E9QJ73, O00254, O08675, O46685, P0C0W8, P0C5J4, P32246, P32249, P32250, P34996, P35366, P35383, P41231, P41232, P46093, P47900, P48042, P49650, P49651, P49652, P50132, P56482, P58826, P59902, P79928, P97266, Q149R9, Q15743, Q1JQB3, Q2Y2P0, Q3U6B2, Q3ZC80, Q4G072, Q4KLH9, Q5E9H8

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
P2RY2	“up-regulates activity”	GNAS	binding
P2RY2	“up-regulates activity”	GNAL	binding
P2RY2	“up-regulates activity”	GNA15	binding
P2RY2	“up-regulates activity”	GNA12	binding
P2RY2	“up-regulates activity”	GNA13	binding
ATP(4-)	“up-regulates activity”	P2RY2	“chemical activation”
P2RY2	“up-regulates activity”	H3-3A	demethylation
P2RY2	“up-regulates activity”	“Histone H3”	demethylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	69
Likely benign	5
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

827 predictions. Top by Δscore:

Variant	Effect	Δscore
11:73234154:AGGGC:A	acceptor_gain	0.9900
11:73234155:GGGCG:G	acceptor_gain	0.9900
11:73234154:AG:A	acceptor_gain	0.9800
11:73234155:GG:G	acceptor_gain	0.9800
11:73234150:CTGCA:C	acceptor_loss	0.9700
11:73234151:TGCA:T	acceptor_loss	0.9700
11:73234152:GCA:G	acceptor_loss	0.9700
11:73234153:CA:C	acceptor_loss	0.9700
11:73234154:A:AG	acceptor_gain	0.9700
11:73234154:A:C	acceptor_loss	0.9700
11:73234155:G:GC	acceptor_loss	0.9700
11:73234155:G:GG	acceptor_gain	0.9700
11:73234155:GGGC:G	acceptor_gain	0.9700
11:73218410:G:GT	donor_gain	0.9600
11:73228172:TCAG:T	donor_loss	0.9600
11:73228173:CAG:C	donor_loss	0.9600
11:73228175:GGTA:G	donor_loss	0.9600
11:73228176:GTAC:G	donor_loss	0.9600
11:73228177:T:A	donor_loss	0.9600
11:73234154:AGG:A	acceptor_gain	0.9600
11:73234155:GGG:G	acceptor_gain	0.9600
11:73218408:G:GT	donor_gain	0.9300
11:73218427:C:T	donor_gain	0.9300
11:73234151:T:TA	acceptor_gain	0.9200
11:73228137:GCGC:G	donor_gain	0.9100
11:73228178:AC:A	donor_loss	0.9100
11:73218311:G:T	donor_gain	0.9000
11:73218409:A:T	donor_gain	0.8800
11:73228158:A:T	donor_gain	0.8800
11:73228075:GA:G	acceptor_gain	0.8700

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000299151 (11:73217554 G>A,C), RS1000587609 (11:73223243 C>A), RS1000723192 (11:73217286 C>A,T), RS1000781398 (11:73235647 A>C), RS1000833248 (11:73240090 T>A), RS1000979468 (11:73223029 A>G), RS1001049347 (11:73229304 C>T), RS1001053775 (11:73223615 T>C), RS1001081518 (11:73241706 C>T), RS1001316375 (11:73232788 G>C), RS1001571208 (11:73238836 T>C), RS1001751157 (11:73239055 T>C), RS1001788165 (11:73234563 T>C), RS1001821677 (11:73238619 A>G), RS1001828063 (11:73227781 G>A,C,T)

Disease associations

OMIM: gene MIM:600041 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

19 associations (top):

Study	Trait	p-value
GCST001586_1	Insomnia (caffeine-induced)	8.000000e-06
GCST001945_5	Body mass index in asthmatics	8.000000e-06
GCST002726_40	Glucose homeostasis traits	4.000000e-06
GCST003599_3	Systemic lupus erythematosus	7.000000e-11
GCST004618_34	White blood cell count (basophil)	5.000000e-27
GCST004631_53	Basophil percentage of white cells	1.000000e-25
GCST004634_38	Basophil percentage of granulocytes	2.000000e-23
GCST008295_20	Number of decayed, missing and filled tooth surfaces or use of dentures	3.000000e-08
GCST008306_2	Dentures	2.000000e-06
GCST90002379_91	Basophil count	3.000000e-24
GCST90002379_92	Basophil count	6.000000e-64
GCST90002380_100	Basophil percentage of white cells	3.000000e-21
GCST90002380_101	Basophil percentage of white cells	4.000000e-70
GCST90002393_435	Monocyte count	2.000000e-16
GCST90002394_471	Monocyte percentage of white cells	2.000000e-15
GCST90002401_184	Platelet distribution width	3.000000e-19
GCST90002401_185	Platelet distribution width	2.000000e-12
GCST90013663_79	Alanine aminotransferase levels	1.000000e-08
GCST90013664_75	Aspartate aminotransferase levels	5.000000e-08

EFO canonical traits (11, from GWAS)

EFO ID	Trait name
EFO:0007876	insomnia measurement
EFO:0004340	body mass index
EFO:0006831	acute insulin response measurement
EFO:0005090	basophil count
EFO:0007992	basophil percentage of leukocytes
EFO:0007995	basophil percentage of granulocytes
EFO:0010078	dentures
EFO:0005091	monocyte count
EFO:0007989	monocyte percentage of leukocytes
EFO:0007984	platelet component distribution width
EFO:0004736	aspartate aminotransferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4398 (SINGLE PROTEIN), CHEMBL4524011 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 508,522 (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
CHEMBL1767408	DIQUAFOSOL TETRASODIUM	4	341
CHEMBL221326	DIQUAFOSOL	4	413
CHEMBL752	ADENOSINE PHOSPHATE	4	165,316
CHEMBL1767407	DENUFOSOL TETRASODIUM	3	270
CHEMBL265502	SURAMIN	3	36,848
CHEMBL336296	URIDINE TRIPHOSPHATE	3	17,782
CHEMBL507282	DENUFOSOL	3	199
CHEMBL14249	ADENOSINE TRIPHOSPHATE	2	287,353

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — P2Y receptors

Most potent curated ligand interactions (17 total), top 17:

Ligand	Action	Affinity	Parameter
MRS2698	Full agonist	8.1	pEC50
UTP	Full agonist	8.1	pEC50
4-thio-UTP	Full agonist	7.5	pEC50
2-thioUTP	Agonist	7.3	pEC50
ATP	Full agonist	7.1	pEC50
diquafosol	Full agonist	7.0	pEC50
PSB1114	Full agonist	6.9	pEC50
denufosol	Full agonist	6.7	pEC50
Ap4A	Full agonist	6.1	pEC50
AR-C126313	Antagonist	6.0	pEC50
reactive blue-2	Antagonist	6.0	pIC50
AR-C118925XX	Antagonist	6.0	pIC50
UTPγS	Full agonist	5.8	pEC50
5BrUTP	Full agonist	5.7	pEC50
MRS2768	Full agonist	5.7	pEC50
PSB-416	Antagonist	4.66	pIC50
suramin	Antagonist	4.3	pIC50

ChEMBL bioactivities

444 potent at pChembl≥5 of 505 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.52	EC50	3	nM	CHEMBL427685
8.52	EC50	3	nM	CHEMBL241483
8.50	Kd	3.162	nM	CHEMBL4066222
8.40	EC50	4	nM	CHEMBL239573
8.30	EC50	5	nM	CHEMBL399017
8.25	EC50	5.61	nM	URIDINE TRIPHOSPHATE
8.22	EC50	6	nM	CHEMBL238542
8.15	EC50	7	nM	URIDINE TRIPHOSPHATE
8.15	EC50	7	nM	CHEMBL392989
8.10	EC50	8	nM	CHEMBL373780
8.10	EC50	8	nM	CHEMBL241482
8.10	EC50	8	nM	N-METHANOCARBA-UTP
8.00	Kd	10	nM	CHEMBL4086462
8.00	EC50	10	nM	CHEMBL240201
8.00	EC50	10	nM	CHEMBL391317
7.92	EC50	12	nM	CHEMBL240202
7.90	Kd	12.59	nM	CHEMBL4090014
7.89	EC50	13	nM	CHEMBL393741
7.80	Kd	15.85	nM	CHEMBL4084674
7.80	Kd	15.85	nM	CHEMBL4082045
7.80	EC50	16	nM	CHEMBL391663
7.80	EC50	15.9	nM	N-METHANOCARBA-UTP
7.80	EC50	16	nM	CHEMBL1083763
7.75	EC50	17.9	nM	URIDINE TRIPHOSPHATE
7.70	Kd	19.95	nM	CHEMBL4073600
7.70	EC50	20	nM	URIDINE TRIPHOSPHATE
7.66	Ki	21.88	nM	CHEMBL4082045
7.66	EC50	22	nM	CHEMBL241481
7.60	Kd	25.12	nM	CHEMBL4089252
7.58	EC50	26	nM	CHEMBL399018
7.58	EC50	26	nM	CHEMBL1767409
7.55	EC50	28	nM	CHEMBL1198849
7.52	EC50	30	nM	URIDINE TRIPHOSPHATE
7.52	EC50	30	nM	CHEMBL239815
7.52	EC50	30	nM	CHEMBL503798
7.52	EC50	30.1	nM	ADENOSINE TRIPHOSPHATE
7.51	EC50	31	nM	CHEMBL393100
7.50	Kd	31.62	nM	CHEMBL4068069
7.49	Ki	32.36	nM	CHEMBL4082045
7.47	EC50	34	nM	CHEMBL406266
7.46	EC50	35	nM	CHEMBL217803
7.46	EC50	35	nM	CHEMBL241318
7.46	EC50	35	nM	CHEMBL428387
7.45	Ki	35.48	nM	CHEMBL4082045
7.43	EC50	37.2	nM	URIDINE TRIPHOSPHATE
7.40	Kd	39.81	nM	CHEMBL4099908
7.38	Ki	41.69	nM	CHEMBL4082045
7.38	EC50	42	nM	CHEMBL238957
7.37	EC50	43	nM	URIDINE TRIPHOSPHATE
7.36	EC50	44	nM	CHEMBL1162198

PubChem BioAssay actives

446 with measured affinity, of 1156 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
bis[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] hydrogen phosphate	261699: Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase	ec50	<0.0001	uM
bis[[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate	261699: Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase	ec50	<0.0001	uM
70681486	261699: Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase	ec50	<0.0001	uM
70683604	261699: Activity against human P2Y2-GFP expressed in A549 cells by intracellular calcium increase	ec50	<0.0001	uM
[[(2R,3S,4R,5R)-5-(5-fluoro-1,3-benzothiazol-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0030	uM
[[(2R,3S,4R,5R)-5-(7-fluoro-6-methylsulfanyl-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0030	uM
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-sulfanylidene-5-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenyl)pyrimidin-1-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0032	uM
[[(2R,3S,4R,5R)-5-[6-(dimethylamino)-7-fluoro-1-oxoisoquinolin-2-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0040	uM
[[(2R,3S,4R,5R)-5-(7-fluoro-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0050	uM
[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1465367: Agonist activity at wild type P2Y2 receptor (unknown origin) expressed in human 1321N1 astrocytoma cells assessed as increase in intracellular calcium mobilization after 1 hr by Fluo-4 AM dye based fluorescence assay	ec50	0.0056	uM
[[(2R,3S,4R,5R)-5-(7-fluoro-6-methoxy-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0060	uM
[[(2R,3S,4R,5R)-5-(6-chloro-4-fluoro-1,3-benzothiazol-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0070	uM
[[(1R,2R,3S,4R,5S)-4-(2,4-dioxopyrimidin-1-yl)-2,3-dihydroxy-1-bicyclo[3.1.0]hexanyl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	150498: Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell	ec50	0.0080	uM
[[(2R,3S,4R,5R)-4-amino-3-hydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	280297: Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C	ec50	0.0080	uM
[[(2R,3S,4R,5R)-5-(6-chloro-1,3-benzothiazol-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0080	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0100	uM
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-sulfanylidene-5-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenyl)pyrimidin-1-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0100	uM
[[(2R,3S,4R,5R)-5-(7-chloro-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0100	uM
[[(2R,3S,4R,5R)-5-(7-cyano-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0120	uM
tetrasodium;[[(2R,3S,4R,5R)-5-[5-[bis(4-chlorophenyl)methyl]-2-oxo-4-sulfanylidenepyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-[dichloro(phosphonato)methyl]phosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0126	uM
[[(2R,3S,4R,5R)-5-(6,7-dichloro-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0130	uM
tetrasodium;[[(2R,3S,4R,5R)-5-[5-[bis(4-methylphenyl)methyl]-2-oxo-4-sulfanylidenepyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-[dichloro(phosphonato)methyl]phosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0158	uM
5-[[5-(6,13-dimethyl-2-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaenyl)-2-oxo-4-sulfanylidenepyrimidin-1-yl]methyl]-N-(2H-tetrazol-5-yl)furan-2-carboxamide	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0158	uM
[[(2R,3S,4R,5R)-5-(6,7-difluoro-1-oxoisoquinolin-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0160	uM
[[(1S,2S,4S,5S)-4-(2,4-dioxopyrimidin-1-yl)-2-hydroxy-1-bicyclo[3.1.0]hexanyl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	484783: Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay	ec50	0.0160	uM
tetrasodium;[[(2R,3S,4R,5R)-5-[5-[bis(3,4-dichlorophenyl)methyl]-2-oxo-4-sulfanylidenepyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-[dichloro(phosphonato)methyl]phosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0199	uM
[[(2R,3S,4R,5R)-5-(1,3-benzothiazol-2-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0220	uM
(2S)-2-[[5-[[5-(6,13-dimethyl-2-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaenyl)-2-oxo-4-sulfanylidenepyrimidin-1-yl]methyl]furan-2-carbonyl]amino]butanedioic acid	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0251	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	593124: Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay	ec50	0.0260	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(7-methoxy-1-oxoisoquinolin-2-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0260	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(methoxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1121981: Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis	ec50	0.0280	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxothieno[3,2-c]pyridin-5-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0300	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate	404832: Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay	ec50	0.0300	uM
[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	350683: Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level	ec50	0.0301	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(1-oxoisoquinolin-2-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0310	uM
2-[2-[[5-[[5-(6,13-dimethyl-2-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaenyl)-2-oxo-4-sulfanylidenepyrimidin-1-yl]methyl]furan-2-carbonyl]amino]-1,3-thiazol-4-yl]acetic acid	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0316	uM
tetrasodium;[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2S,3R,4S,5S)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate	315756: Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay	ec50	0.0340	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	280297: Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C	ec50	0.0350	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(5-oxo-1,6-naphthyridin-6-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0350	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(6-methyl-1-oxoisoquinolin-2-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0350	uM
(2S)-2-[[2-[[5-(6,13-dimethyl-2-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaenyl)-2-oxo-4-sulfanylidenepyrimidin-1-yl]methyl]-1,3-thiazole-4-carbonyl]amino]butanedioic acid	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0398	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(6-methoxy-1,3-benzothiazol-2-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	305248: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0420	uM
[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2S,3R,4S,5S)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate	315756: Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay	ec50	0.0440	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[3-(4-methoxyphenyl)propoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1140089: Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting	ec50	0.0470	uM
N,N-diethylethanamine;[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(methoxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	484783: Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay	ec50	0.0500	uM
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-sulfanylidene-5-(9H-xanthen-9-yl)pyrimidin-1-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate	1464911: Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay	kd	0.0501	uM
[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2-benzyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxy-hydroxyphosphoryl] [[[(2S,3R,4S,5S)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate	315756: Agonist activity at P2Y2 receptor expressed in human 1321 cells by calcium mobilization assay	ec50	0.0520	uM
[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(1-oxo-5,6,7,8-tetrahydroisoquinolin-2-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	304928: Agonist activity at human P2Y2 receptor expressed in human 1321N1 by FLIPR assay	ec50	0.0550	uM
[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate	647894: Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry	ec50	0.0600	uM
[[(2R,3S,4R,5R)-4-amino-5-(2,4-dioxopyrimidin-1-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	280297: Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C	ec50	0.0620	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases abundance, increases expression	5
Tobacco Smoke Pollution	affects expression, decreases expression, increases expression	3
Air Pollutants	increases abundance, decreases expression, affects expression	2
Benzo(a)pyrene	increases methylation, affects methylation, increases expression	2
Calcitriol	increases expression	2
Cisplatin	affects cotreatment, increases expression, decreases expression	2
Nickel	increases expression	2
Silicon Dioxide	increases expression, decreases expression	2
Valproic Acid	affects expression, increases expression	2
Cadmium Chloride	decreases expression	2
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
sodium arsenate	decreases expression, increases abundance	1
arsenite	decreases expression, increases abundance	1
sulforaphane	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
cobaltous chloride	increases expression	1
butyraldehyde	increases expression	1
monomethylarsonic acid	decreases expression	1
arsenic acid	decreases expression, increases abundance	1
vanadyl sulfate	decreases expression	1
pentanal	increases expression	1
di-n-butylphosphoric acid	affects expression	1
N-butyrylhomoserine lactone	decreases expression	1
N-(3-oxododecanoyl)homoserine lactone	decreases expression, decreases reaction	1
monomethylarsonous acid	decreases expression	1
abrine	decreases expression	1
dimethylmonothioarsinic acid	decreases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	increases response to substance, decreases expression	1

ChEMBL screening assays

219 unique, capped per target: 160 functional, 59 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1005026	Functional	Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis	Identification of hydrolytically stable and selective P2Y(1) receptor agonists. — Eur J Med Chem
CHEMBL1072551	Binding	Inhibition of human P2Y2 receptor expressed in CHO cells	Identification of a new class of small molecule C5a receptor antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

6 cell lines: 5 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H358	1321N1/P2Y2	Cancer cell line	Male
CVCL_L434	P2UR/K-562	Cancer cell line	Female
CVCL_LB08	PathHunter U2OS P2RY2 Activated GPCR Internalization	Cancer cell line	Female
CVCL_LB09	PathHunter U2OS P2RY2 beta-arrestin	Cancer cell line	Female
CVCL_ZD91	1321N1-HA-P2Y2	Cancer cell line	Male
CVCL_ZK58	GeneBLAzer P2RY2-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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