P2RY4
geneOn this page
Also known as NRUP2Y4UNRP2P
Summary
P2RY4 (pyrimidinergic receptor P2Y4, HGNC:8542) is a protein-coding gene on chromosome Xq13.1, encoding P2Y purinoceptor 4 (P51582). Receptor for UTP and UDP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system.
The product of this gene belongs to the family of 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 is responsive to uridine nucleotides, partially responsive to ATP, and not responsive to ADP.
Source: NCBI Gene 5030 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 55 total
- Druggable target: yes — 6 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002565
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:8542 |
| Approved symbol | P2RY4 |
| Name | pyrimidinergic receptor P2Y4 |
| Location | Xq13.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | NRU, P2Y4, UNR, P2P |
| Ensembl gene | ENSG00000186912 |
| Ensembl biotype | protein_coding |
| OMIM | 300038 |
| Entrez | 5030 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000374519
RefSeq mRNA: 1 — MANE Select: NM_002565
NM_002565
CCDS: CCDS14398
Canonical transcript exons
ENST00000374519 — 1 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001463714 | 70258166 | 70260204 |
Expression profiles
Bgee: expression breadth broad, 77 present calls, max score 64.21.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0468 / max 5.9022, expressed in 24 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 199527 | 0.0468 | 24 |
Top tissues by expression
249 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| tibialis anterior | UBERON:0001385 | 64.21 | gold quality |
| ileal mucosa | UBERON:0000331 | 62.91 | gold quality |
| cranial nerve II | UBERON:0000941 | 59.55 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 57.09 | gold quality |
| pancreatic ductal cell | CL:0002079 | 56.68 | silver quality |
| decidua | UBERON:0002450 | 56.55 | gold quality |
| small intestine | UBERON:0002108 | 56.01 | gold quality |
| deltoid | UBERON:0001476 | 54.65 | silver quality |
| skin of abdomen | UBERON:0001416 | 53.42 | gold quality |
| hair follicle | UBERON:0002073 | 52.43 | gold quality |
| rectum | UBERON:0001052 | 52.14 | gold quality |
| skin of leg | UBERON:0001511 | 51.96 | gold quality |
| zone of skin | UBERON:0000014 | 51.38 | gold quality |
| skin of hip | UBERON:0001554 | 50.68 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 50.62 | gold quality |
| quadriceps femoris | UBERON:0001377 | 49.79 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 49.30 | gold quality |
| blood vessel layer | UBERON:0004797 | 49.29 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 49.20 | gold quality |
| olfactory bulb | UBERON:0002264 | 48.92 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 48.89 | gold quality |
| myocardium | UBERON:0002349 | 48.87 | gold quality |
| type B pancreatic cell | CL:0000169 | 48.83 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 48.55 | gold quality |
| CA1 field of hippocampus | UBERON:0003881 | 48.50 | gold quality |
| vastus lateralis | UBERON:0001379 | 48.38 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 48.24 | gold quality |
| orbitofrontal cortex | UBERON:0004167 | 48.20 | gold quality |
| upper leg skin | UBERON:0004262 | 48.10 | silver quality |
| upper arm skin | UBERON:0004263 | 48.06 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.47 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): EZH2, MYOD1, STAT2, TP53, TP73
miRNA regulators (miRDB)
26 targeting P2RY4, 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-6833-3P | 100.00 | 70.63 | 3197 |
| HSA-MIR-4768-5P | 100.00 | 69.49 | 2861 |
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-4725-3P | 99.96 | 69.53 | 2520 |
| HSA-MIR-6780B-5P | 99.96 | 69.60 | 2562 |
| HSA-MIR-4271 | 99.88 | 68.32 | 2244 |
| HSA-MIR-6124 | 99.87 | 69.78 | 3551 |
| HSA-MIR-4447 | 99.85 | 67.81 | 2900 |
| HSA-MIR-6752-3P | 99.72 | 66.71 | 1587 |
| HSA-MIR-4472 | 99.56 | 66.08 | 1478 |
| HSA-MIR-1275 | 99.47 | 67.90 | 2749 |
| HSA-MIR-4695-5P | 99.06 | 64.87 | 1151 |
| HSA-MIR-625-5P | 99.02 | 68.64 | 2031 |
| HSA-MIR-4699-5P | 98.99 | 67.50 | 1210 |
| HSA-MIR-583 | 98.71 | 67.44 | 1791 |
| HSA-MIR-4700-5P | 98.63 | 67.43 | 1915 |
| HSA-MIR-4712-3P | 98.52 | 65.39 | 822 |
| HSA-MIR-3179 | 98.22 | 65.90 | 1445 |
| HSA-MIR-34C-3P | 98.11 | 65.60 | 858 |
| HSA-MIR-8089 | 97.74 | 66.21 | 1698 |
| HSA-MIR-3936 | 97.64 | 64.47 | 732 |
| HSA-MIR-4667-5P | 97.61 | 66.67 | 1683 |
| HSA-MIR-3173-5P | 97.35 | 65.82 | 1282 |
| HSA-MIR-6799-3P | 97.35 | 65.60 | 1302 |
| HSA-MIR-3116 | 97.07 | 65.78 | 1324 |
| HSA-MIR-874-5P | 96.93 | 63.92 | 1014 |
Literature-anchored findings (GeneRIF, showing 9)
- 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)
- Activation of the human P2Y(4) receptor expressed in 1321N1 cells by UTP did not elicit this protective effect, although both receptors were coupled to phospholipase C. (PMID:12623123)
- second extracellular loop and the NH(2) terminus form a functional motif that plays a key role in determining whether ATP functions as an agonist or antagonist at mammalian P2Y(4) receptors (PMID:14670966)
- Taken together, our data indicate that the high expression and activation of the P2Y4 receptor participates in the neuronal differentiation and commitment to death of SH-SY5Y cells. (PMID:15649700)
- Nucleotide P2Y4 receptor binding is arrested in post-Golgi trafficking by type I transmembrane proteins p23 and p24A. (PMID:21219331)
- P2Y4 receptors are expressed in intracellular vesicles and sarcolemma of skeletal muscle fibers. (PMID:22052557)
- show that P2 receptors and protein kinases are also involved in regulating injury-induced expression and the release of TSP-1 in injured astrocytes (PMID:22776902)
- reflected in the immunoblotting data P2RY4 receptors were detected at higher levels of expression in patient with cortical dysplasia with intractable epilepsy. (PMID:25003238)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | P2ry4 | ENSMUSG00000044359 |
| rattus_norvegicus | P2ry4 | ENSRNOG00000070777 |
Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR2 (ENSG00000126262), FFAR1 (ENSG00000126266), OXER1 (ENSG00000162881), OXGR1 (ENSG00000165621), P2RY1 (ENSG00000169860), P2RY6 (ENSG00000171631), GPR82 (ENSG00000171657), P2RY2 (ENSG00000175591), HCAR2 (ENSG00000182782), FFAR3 (ENSG00000185897), HCAR1 (ENSG00000196917), SUCNR1 (ENSG00000198829), HCAR3 (ENSG00000255398)
Protein
Protein identifiers
P2Y purinoceptor 4 — P51582 (reviewed: P51582)
Alternative names: P2P, Uridine nucleotide receptor
All UniProt accessions (1): P51582
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for UTP and UDP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system. Not activated by ATP or ADP.
Subcellular location. Cell membrane.
Tissue specificity. Pancreas.
Post-translational modifications. Phosphorylation of Ser-333 and Ser-334 is a key step in agonist-dependent desensitization and loss of surface P2RY4. This phosphorylation does not involve PKC, nor other calcium activated kinases.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (1): NP_002556* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000018 | P2Y4 | Family |
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
Pfam: PF00001
UniProt features (35 total): topological domain 8, mutagenesis site 8, transmembrane region 7, sequence variant 4, sequence conflict 4, modified residue 2, chain 1, disulfide bond 1
Structure
Experimental structures (PDB)
1 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9K0K | ELECTRON MICROSCOPY | 3.14 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P51582-F1 | 83.60 | 0.66 |
Antibody-complex structures (SAbDab): 1 — 9K0K
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (2): 333, 334
Disulfide bonds (1): 108–185
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 243 | no effect. |
| 333–365 | abolishes agonist-induced phosphorylation. prevents agonist-induced desensitization and loss of cell surface receptors. |
| 333–359 | greatly reduces agonist-induced desensitization and loss of cell surface receptors. |
| 333 | greatly reduces agonist-induced desensitization and loss of cell surface receptors; when associated with a-334 and a-339 |
| 334 | greatly reduces agonist-induced desensitization and loss of cell surface receptors; when associated with a-333 and a-339 |
| 339 | greatly reduces agonist-induced desensitization and loss of cell surface receptors; when associated with a-333 and a-334 |
| 344–365 | no effect on agonist-induced phosphorylation, no functional effect. |
| 356–365 | no functional effect. |
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-417957 | P2Y receptors |
| R-HSA-418594 | G alpha (i) signalling events |
MSigDB gene sets: 86 (showing top):
GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, GOBP_RESPONSE_TO_PROSTAGLANDIN_E, GOBP_CELLULAR_RESPONSE_TO_LIPID, XU_HGF_TARGETS_REPRESSED_BY_AKT1_DN, REACTOME_P2Y_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_PROSTAGLANDIN_STIMULUS, GOBP_INORGANIC_ANION_TRANSPORT, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, CAGCTG_AP4_Q5, GOBP_CELLULAR_RESPONSE_TO_ATP, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_RESPONSE_TO_PROSTAGLANDIN, GOBP_CHLORIDE_TRANSPORT, GOBP_RESPONSE_TO_KETONE
GO Biological Process (8): G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), transepithelial chloride transport (GO:0030321), cellular response to ATP (GO:0071318), cellular response to prostaglandin E stimulus (GO:0071380), signal transduction (GO:0007165), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589)
GO Molecular Function (4): 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-2 pathways:
| Category | Pathways |
|---|---|
| Nucleotide-like (purinergic) receptors | 1 |
| GPCR downstream signalling | 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 |
| signal transduction | 1 |
| phospholipase C activator activity | 1 |
| regulation of biological quality | 1 |
| chloride transport | 1 |
| transepithelial transport | 1 |
| response to ATP | 1 |
| cellular response to nitrogen compound | 1 |
| cellular response to oxygen-containing compound | 1 |
| response to prostaglandin E | 1 |
| cellular response to prostaglandin stimulus | 1 |
| cellular response to alcohol | 1 |
| cellular response to ketone | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| purinergic nucleotide receptor signaling pathway | 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
402 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| P2RY4 | P2RX1 | P51575 | 889 |
| P2RY4 | P2RX2 | Q9UBL9 | 863 |
| P2RY4 | PPAN | Q9NQ55 | 826 |
| P2RY4 | P2RX6 | O15547 | 804 |
| P2RY4 | P2RX5 | Q93086 | 803 |
| P2RY4 | P2RX3 | P56373 | 775 |
| P2RY4 | P2RX4 | Q99571 | 756 |
| P2RY4 | P2RX7 | Q99572 | 689 |
| P2RY4 | GNAQ | P50148 | 684 |
| P2RY4 | ENTPD8 | Q5MY95 | 583 |
| P2RY4 | ENTPD1 | P49961 | 581 |
| P2RY4 | ENTPD3 | O75355 | 572 |
| P2RY4 | P2RY2 | P41231 | 569 |
| P2RY4 | P2RY11 | Q96G91 | 566 |
| P2RY4 | A0A0B4J1V8 | A0A0B4J1V8 | 564 |
IntAct
6 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| P2RY4 | OPTN | psi-mi:“MI:0915”(physical association) | 0.560 |
| P2RY4 | TMED2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GOLPH3 | P2RY4 | psi-mi:“MI:0915”(physical association) | 0.400 |
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: A5PLE7, B0UXR0, B5X337, D4A7K7, F1MV99, O08858, O35210, O35811, O77590, O88634, P11613, P21556, P25025, P25095, P25104, P25106, P26824, P29089, P29754, P29755, P30555, P30556, P30937, P30938, P31391, P32249, P32250, P32300, P33396, P33535, P34976, P35346, P35366, P35372, P35373, P35383, P41143, P41231, P41232, P42866
SIGNOR signaling
7 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| P2RY4 | “up-regulates activity” | GNAI1 | binding |
| P2RY4 | “up-regulates activity” | GNAI3 | binding |
| P2RY4 | “up-regulates activity” | GNAO1 | binding |
| P2RY4 | “up-regulates activity” | GNAZ | binding |
| P2RY4 | “up-regulates activity” | GNA15 | binding |
| P2RY4 | “up-regulates activity” | GNA13 | binding |
| ATP(4-) | “up-regulates activity” | P2RY4 | “chemical activation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
55 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 52 |
| Likely benign | 1 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
160 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| X:70258657:C:CT | donor_gain | 0.7600 |
| X:70258653:G:A | donor_gain | 0.7500 |
| X:70258564:T:A | donor_gain | 0.7100 |
| X:70258658:C:CT | donor_gain | 0.7100 |
| X:70258652:TGCC:T | donor_gain | 0.7000 |
| X:70258786:A:AC | donor_gain | 0.6800 |
| X:70258787:C:CC | donor_gain | 0.6800 |
| X:70258801:T:TA | donor_gain | 0.6700 |
| X:70258654:C:CT | donor_gain | 0.6600 |
| X:70258672:CGGAG:C | donor_gain | 0.6600 |
| X:70258676:G:C | donor_gain | 0.6300 |
| X:70258753:G:C | donor_gain | 0.6100 |
| X:70258679:G:T | donor_gain | 0.5900 |
| X:70258682:G:C | donor_gain | 0.5900 |
| X:70258837:A:AC | acceptor_gain | 0.5700 |
| X:70258660:C:CT | donor_gain | 0.5600 |
| X:70258667:G:C | donor_gain | 0.5600 |
| X:70258766:C:CT | donor_gain | 0.5600 |
| X:70258597:T:TA | donor_gain | 0.5500 |
| X:70258670:G:T | donor_gain | 0.5500 |
| X:70258513:C:A | donor_gain | 0.5400 |
| X:70258756:A:AC | donor_gain | 0.5000 |
| X:70258757:C:CC | donor_gain | 0.5000 |
| X:70258837:A:C | acceptor_gain | 0.5000 |
| X:70258512:T:TA | donor_gain | 0.4900 |
| X:70258521:C:A | donor_gain | 0.4900 |
| X:70258767:C:CT | donor_gain | 0.4800 |
| X:70258937:GCT:G | acceptor_gain | 0.4800 |
| X:70258651:TTGC:T | donor_gain | 0.4700 |
| X:70258877:C:CT | donor_gain | 0.4700 |
AlphaMissense
2339 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| X:70259235:G:C | S130R | 0.997 |
| X:70259235:G:T | S130R | 0.997 |
| X:70259237:T:G | S130R | 0.997 |
| X:70259071:C:G | C185S | 0.996 |
| X:70259072:A:T | C185S | 0.996 |
| X:70259322:C:A | W101C | 0.996 |
| X:70259322:C:G | W101C | 0.996 |
| X:70258851:G:C | F258L | 0.995 |
| X:70258851:G:T | F258L | 0.995 |
| X:70258853:A:G | F258L | 0.995 |
| X:70258737:A:C | S296R | 0.994 |
| X:70258737:A:T | S296R | 0.994 |
| X:70258739:T:G | S296R | 0.994 |
| X:70258842:G:C | F261L | 0.994 |
| X:70258842:G:T | F261L | 0.994 |
| X:70258844:A:G | F261L | 0.994 |
| X:70259502:G:C | S41R | 0.994 |
| X:70259502:G:T | S41R | 0.994 |
| X:70259504:T:G | S41R | 0.994 |
| X:70259383:T:A | D81V | 0.993 |
| X:70258728:G:C | S299R | 0.992 |
| X:70258728:G:T | S299R | 0.992 |
| X:70258730:T:G | S299R | 0.992 |
| X:70258747:G:C | P293R | 0.992 |
| X:70258831:C:G | R265P | 0.992 |
| X:70259280:G:C | F115L | 0.992 |
| X:70259280:G:T | F115L | 0.992 |
| X:70259282:A:G | F115L | 0.992 |
| X:70258863:A:C | F254L | 0.991 |
| X:70258863:A:T | F254L | 0.991 |
dbSNP variants (sampled 300 via entrez): RS1000313857 (X:70261719 C>T), RS1003202581 (X:70262176 C>T), RS1006048686 (X:70260360 C>A), RS1008944839 (X:70260825 C>T), RS1008997147 (X:70261295 A>G), RS1009168180 (X:70260760 G>C), RS1009331848 (X:70258978 G>A,C), RS1009526585 (X:70261153 T>C), RS1010340596 (X:70258066 G>A), RS1011468922 (X:70259707 A>G,T), RS1012969594 (X:70260567 C>A,T), RS1013020718 (X:70260240 G>A), RS1014969284 (X:70262184 C>T), RS1016581957 (X:70258665 G>T), RS1016682011 (X:70260208 C>T)
Disease associations
OMIM: gene MIM:300038 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2123 (SINGLE PROTEIN), CHEMBL4524011 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 306,358 (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 |
| CHEMBL1767407 | DENUFOSOL TETRASODIUM | 3 | 270 |
| 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 (16 total), top 16:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| MRS4062 | Full agonist | 7.6 | pEC50 |
| MRS2927 | Full agonist | 7.21 | pEC50 |
| N4-phenylethoxycytidine-5’-triphosphate | Full agonist | 7.14 | pEC50 |
| (N)methanocarba-UTP | Full agonist | 7.1 | pEC50 |
| PSB-16133 | Antagonist | 6.63 | pIC50 |
| diquafosol | Full agonist | 6.4 | pEC50 |
| UTP | Full agonist | 6.3 | pEC50 |
| denufosol | Full agonist | 6.1 | pEC50 |
| Ap4A | Partial agonist | 5.9 | pEC50 |
| ATP | Agonist | 5.37 | pEC50 |
| 2-amino-uridine-5’-monophosphate | Partial agonist | 5.3 | pEC50 |
| guanosine-5’-triphosphate | Partial agonist | 5.2 | pEC50 |
| CTP | Partial agonist | 5.1 | pEC50 |
| ITP | Partial agonist | 5.1 | pEC50 |
| PPADS | Antagonist | 5.0 | pEC50 |
| reactive blue-2 | Antagonist | 4.7 | pIC50 |
ChEMBL bioactivities
209 potent at pChembl≥5 of 230 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
208 with measured affinity, of 588 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 |
|---|---|---|---|---|
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-thiophen-3-ylpropoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0200 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 593125: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay | ec50 | 0.0230 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-phenylpropoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.0230 | 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 | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0230 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(methoxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1121979: Agonist activity at human recombinant P2Y4 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 | 0.0250 | uM |
| [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 304930: Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay | ec50 | 0.0390 | uM |
| [[(2R,3S,4R,5R)-5-[4-[3-[4-[2-(but-3-ynylamino)-2-oxoethoxy]phenyl]propoxyamino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0400 | uM |
| [[(2R,3S,4R,5R)-5-[4-[(3-cyano-3,3-diphenylpropoxy)amino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0470 | 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 | 150625: Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell | ec50 | 0.0490 | 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 | 484777: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay | ec50 | 0.0500 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(4-phenylbutoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0540 | uM |
| [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4S,5R,6R)-4-fluoro-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.0620 | uM |
| [[(2R,3S,4R,5R)-5-[4-[3-[4-[2-[2-[1-[3-[6-[[2-[4-[(E)-2-(2,2-difluoro-12-thiophen-2-yl-3-aza-1-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-1(12),4,6,8,10-pentaen-4-yl)ethenyl]phenoxy]acetyl]amino]hexanoylamino]propyl]triazol-4-yl]ethylamino]-2-oxoethoxy]phenyl]propoxyamino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0700 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(2-phenylethoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.0730 | 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 | 404834: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | ec50 | 0.0800 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[3-(4-nitrophenyl)propoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0840 | uM |
| [[(1S,2S,4S,5S)-4-(2,4-dioxopyrimidin-1-yl)-2-hydroxy-1-bicyclo[3.1.0]hexanyl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 484777: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay | ec50 | 0.0850 | uM |
| [dichloro-[[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid | 404834: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | ec50 | 0.0900 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[3-(4-iodophenyl)propoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0910 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-phenylpropoxyamino)pyrimidin-1-yl]oxolan-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 | 1140103: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay | ec50 | 0.0930 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[3-(3-nitrophenyl)propoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.0950 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(phenylmethoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1121979: Agonist activity at human recombinant P2Y4 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 | 0.0970 | uM |
| [[(2R,3S,4R,5R)-5-[4-[3-(3-fluorophenyl)propoxyamino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.1000 | uM |
| [[(2R,3S,4R,5R)-5-[4-[3-(4-fluorophenyl)propoxyamino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.1050 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[3-(3-iodophenyl)propoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.1140 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(3-naphthalen-2-ylpropoxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.1280 | uM |
| tetrasodium;[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.1300 | 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 | 280298: Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | ec50 | 0.1300 | uM |
| [[(2R,3S,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxyoxolan-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 | 404834: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | ec50 | 0.1400 | uM |
| [[(2R,3S,4R,5R)-5-[4-[3-(4-bromophenyl)propoxyamino]-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.1410 | uM |
| N,N-diethylethanamine;[(2R,3S,4R,5R)-5-[4-(ethoxyamino)-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate | 484777: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay | ec50 | 0.1800 | uM |
| [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [hydroxy-[hydroxy-[(2R,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphosphoryl]oxyphosphoryl] hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.1830 | uM |
| 2-(3-amino-6-imino-4,5-disulfoxanthen-9-yl)-5-[6-[4-[2-[[2-[4-[3-[[1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[[hydroxy-[hydroxy(phosphonooxy)phosphoryl]oxyphosphoryl]oxymethyl]oxolan-2-yl]-2-oxopyrimidin-4-yl]amino]oxypropyl]phenoxy]acetyl]amino]ethyl]triazol-1-yl]hexylcarbamoyl]benzoic acid;bis(N,N-diethylethanamine) | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.2000 | uM |
| [[(2R,3S,4R,5R)-5-[4-(ethoxyamino)-2-oxopyrimidin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.2100 | uM |
| [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3R,4R,5S,6R)-5-fluoro-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.2200 | uM |
| (2S,3S,4S,5R,6R)-6-[[[[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.2270 | uM |
| sodium 1-amino-4-[4-(2,4-dimethylphenyl)sulfanylanilino]-9,10-dioxoanthracene-2-sulfonate | 1443650: Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay | ic50 | 0.2330 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-pyridin-4-ylpropoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.2500 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] [hydroxy(phosphonooxy)phosphoryl] hydrogen phosphate | 404834: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | ec50 | 0.2800 | uM |
| N,N-diethylethanamine;[[(1S,2R,3R,4S,5S)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-2-bicyclo[3.1.0]hexanyl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 484777: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay | ec50 | 0.3000 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-pyridin-3-ylpropoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.3000 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(methoxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4S,5R,6R)-4-fluoro-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate | 600863: Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ec50 | 0.3100 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 280298: Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | ec50 | 0.3500 | uM |
| [(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-[(3-iodophenyl)methoxyamino]-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl phosphono hydrogen phosphate | 1121979: Agonist activity at human recombinant P2Y4 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 | 0.3520 | uM |
| sodium 1-amino-4-[4-(4-chlorophenoxy)anilino]-9,10-dioxoanthracene-2-sulfonate | 1443650: Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay | ic50 | 0.3730 | uM |
| sodium 1-amino-4-[4-(2,5-dimethylphenyl)sulfanylanilino]-9,10-dioxoanthracene-2-sulfonate | 1443650: Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay | ic50 | 0.3950 | uM |
| [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-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 | 89271: Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor | ec50 | 0.4000 | uM |
| sodium 1-amino-9,10-dioxo-4-[4-(pyridin-3-ylmethylsulfanyl)anilino]anthracene-2-sulfonate | 1443650: Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay | ic50 | 0.4090 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(pent-4-ynoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.4100 | uM |
| [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(2-phenoxyethoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate | 1140090: Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting | ec50 | 0.4300 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | affects methylation, decreases expression, decreases methylation | 2 |
| terbufos | increases methylation | 1 |
| N-butyrylhomoserine lactone | decreases expression | 1 |
| CGP 52608 | increases reaction, affects binding | 1 |
| N-(3-oxododecanoyl)homoserine lactone | decreases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Adenosine Triphosphate | affects binding, increases activity, increases abundance, decreases reaction | 1 |
| Air Pollutants | increases expression | 1 |
| Calcium | decreases reaction, affects binding, increases abundance, increases activity | 1 |
| Copper | affects cotreatment, decreases expression | 1 |
| Fonofos | increases methylation | 1 |
| Parathion | increases methylation | 1 |
| Trichloroethylene | increases activity, decreases activity, affects binding, decreases reaction, increases abundance | 1 |
| Valproic Acid | increases methylation | 1 |
| Sodium Selenite | decreases expression | 1 |
| Okadaic Acid | increases expression | 1 |
ChEMBL screening assays
94 unique, capped per target: 80 functional, 14 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1005027 | Functional | Agonist activity at human P2Y4 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 |
| CHEMBL3270106 | Binding | Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as fluorescence intensity by flow cytometry (FCM) binding assay | 4-Alkyloxyimino derivatives of uridine-5’-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors. — J Med Chem |
Cellosaurus cell lines
6 cell lines: 3 cancer cell line, 2 spontaneously immortalized cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_H359 | 1321N1/P2Y4 | Cancer cell line | Male |
| CVCL_KY76 | PathHunter CHO-K1 P2RY4 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_KZ61 | PathHunter HEK 293 P2RY4 beta-arrestin | Transformed cell line | Female |
| CVCL_LB10 | PathHunter U2OS P2RY4 Activated GPCR Internalization | Cancer cell line | Female |
| CVCL_ZD92 | 1321N1-HA-P2Y4 | Cancer cell line | Male |
| CVCL_ZK59 | GeneBLAzer P2RY4-NFAT-bla CHO-K1 | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Denufosol, Diquafosol, Triphosphate, Uridine Triphosphate