P2RY14
gene geneOn this page
Also known as KIAA0001
Summary
P2RY14 (purinergic receptor P2Y14, HGNC:16442) is a protein-coding gene on chromosome 3q25.1, encoding P2Y purinoceptor 14 (Q15391). Receptor for UDP-glucose and other UDP-sugar coupled to G-proteins.
The product of this gene belongs to the family of G-protein coupled receptors, which contains several receptor subtypes with different pharmacological selectivity for various adenosine and uridine nucleotides. This receptor is a P2Y purinergic receptor for UDP-glucose and other UDP-sugars coupled to G-proteins. It has been implicated in extending the known immune system functions of P2Y receptors by participating in the regulation of the stem cell compartment, and it may also play a role in neuroimmune function. Two transcript variants encoding the same protein have been identified for this gene.
Source: NCBI Gene 9934 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 2 total
- Druggable target: yes
- MANE Select transcript:
NM_014879
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:16442 |
| Approved symbol | P2RY14 |
| Name | purinergic receptor P2Y14 |
| Location | 3q25.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | KIAA0001 |
| Ensembl gene | ENSG00000174944 |
| Ensembl biotype | protein_coding |
| OMIM | 610116 |
| Entrez | 9934 |
Gene structure
Transcript identifiers
Ensembl transcripts: 14 — 14 protein_coding
ENST00000309170, ENST00000424796, ENST00000494668, ENST00000908303, ENST00000908304, ENST00000908305, ENST00000908306, ENST00000908307, ENST00000908308, ENST00000908309, ENST00000908310, ENST00000945445, ENST00000945446, ENST00000945447
RefSeq mRNA: 2 — MANE Select: NM_014879
NM_001081455, NM_014879
CCDS: CCDS3156
Canonical transcript exons
ENST00000309170 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001208977 | 151219535 | 151219642 |
| ENSE00001208984 | 151278287 | 151278542 |
| ENSE00001208990 | 151212117 | 151214340 |
Expression profiles
Bgee: expression breadth ubiquitous, 241 present calls, max score 97.33.
FANTOM5 (CAGE): breadth broad, TPM avg 1.7816 / max 122.6493, expressed in 258 samples.
FANTOM5 promoters (10 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 45135 | 0.8704 | 123 |
| 45139 | 0.4166 | 152 |
| 45136 | 0.2913 | 92 |
| 45128 | 0.0459 | 21 |
| 45131 | 0.0418 | 16 |
| 45130 | 0.0350 | 21 |
| 45129 | 0.0303 | 19 |
| 45140 | 0.0205 | 8 |
| 45133 | 0.0202 | 10 |
| 45132 | 0.0096 | 3 |
Top tissues by expression
275 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| decidua | UBERON:0002450 | 97.33 | gold quality |
| skin of hip | UBERON:0001554 | 90.51 | gold quality |
| endothelial cell | CL:0000115 | 89.95 | gold quality |
| synovial joint | UBERON:0002217 | 89.89 | gold quality |
| upper leg skin | UBERON:0004262 | 89.45 | gold quality |
| calcaneal tendon | UBERON:0003701 | 87.51 | gold quality |
| endometrium | UBERON:0001295 | 87.03 | gold quality |
| mucosa of stomach | UBERON:0001199 | 85.70 | gold quality |
| colonic epithelium | UBERON:0000397 | 83.42 | gold quality |
| visceral pleura | UBERON:0002401 | 82.96 | gold quality |
| placenta | UBERON:0001987 | 82.88 | gold quality |
| upper arm skin | UBERON:0004263 | 82.77 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 82.75 | gold quality |
| caecum | UBERON:0001153 | 82.42 | gold quality |
| right lung | UBERON:0002167 | 82.42 | gold quality |
| buccal mucosa cell | CL:0002336 | 82.36 | gold quality |
| rectum | UBERON:0001052 | 81.90 | gold quality |
| vermiform appendix | UBERON:0001154 | 81.70 | gold quality |
| fundus of stomach | UBERON:0001160 | 80.47 | gold quality |
| pleura | UBERON:0000977 | 80.38 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 80.33 | gold quality |
| mammalian vulva | UBERON:0000997 | 79.90 | gold quality |
| superficial temporal artery | UBERON:0001614 | 79.80 | silver quality |
| cardia of stomach | UBERON:0001162 | 79.47 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 79.30 | gold quality |
| oral cavity | UBERON:0000167 | 79.26 | gold quality |
| lower lobe of lung | UBERON:0008949 | 79.16 | gold quality |
| parietal pleura | UBERON:0002400 | 78.77 | gold quality |
| transverse colon | UBERON:0001157 | 78.27 | gold quality |
| body of stomach | UBERON:0001161 | 78.10 | gold quality |
Single-cell (SCXA)
Detected in 7 experiment(s), a significant marker in 7.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-25 | yes | 462.46 |
| E-MTAB-6701 | yes | 115.20 |
| E-MTAB-8498 | yes | 13.50 |
| E-CURD-112 | yes | 12.70 |
| E-HCAD-11 | yes | 9.14 |
| E-MTAB-9801 | yes | 6.78 |
| E-ANND-3 | yes | 4.09 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
89 targeting P2RY14, 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-432-3P | 100.00 | 67.86 | 705 |
| HSA-MIR-4768-5P | 100.00 | 69.49 | 2861 |
| HSA-MIR-34A-5P | 99.99 | 71.21 | 1784 |
| HSA-MIR-449A | 99.99 | 71.05 | 1776 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-34C-5P | 99.97 | 70.45 | 1577 |
| HSA-MIR-449B-5P | 99.97 | 70.26 | 1580 |
| HSA-MIR-507 | 99.97 | 70.11 | 1915 |
| HSA-MIR-570-3P | 99.96 | 72.41 | 4910 |
| HSA-MIR-302E | 99.96 | 70.74 | 2669 |
| HSA-MIR-4666A-3P | 99.96 | 71.71 | 3434 |
| HSA-MIR-557 | 99.96 | 70.01 | 1640 |
| HSA-MIR-9902 | 99.89 | 69.15 | 2250 |
| HSA-MIR-380-3P | 99.89 | 70.18 | 1978 |
| HSA-MIR-302A-3P | 99.89 | 71.23 | 1777 |
| HSA-MIR-302B-3P | 99.89 | 71.23 | 1777 |
| HSA-MIR-302C-3P | 99.89 | 71.20 | 1778 |
| HSA-MIR-302D-3P | 99.89 | 71.25 | 1777 |
| HSA-MIR-373-3P | 99.84 | 70.68 | 1668 |
| HSA-MIR-520E-3P | 99.84 | 70.55 | 1698 |
| HSA-MIR-372-3P | 99.83 | 70.58 | 1691 |
| HSA-MIR-520A-3P | 99.83 | 70.59 | 1687 |
| HSA-MIR-520B-3P | 99.83 | 70.56 | 1699 |
| HSA-MIR-520C-3P | 99.83 | 70.56 | 1699 |
| HSA-MIR-520D-3P | 99.83 | 70.78 | 1676 |
| HSA-MIR-3180-5P | 99.82 | 69.12 | 2422 |
| HSA-MIR-4307 | 99.82 | 70.45 | 3374 |
Literature-anchored findings (GeneRIF, showing 15)
- The IUPHAR Subcommittee for P2Y receptor nomenclature and classification reviews the current knowledge of the UDP-glucose receptor and presents reasons for including it in the P2Y receptor family as the P2Y(14) receptor. (PMID:12559763)
- a G-protein-coupled receptor identifying a quiescent, primitive population of hematopoietic cells restricted to bone marrow; it mediates primitive cell responses to specific hematopoietic microenvironments (PMID:12842911)
- Discrete expression of GPR105 demonstrated within the immature subset of monocyte-derived dendritic cells (DC) suggests a possible role for this receptor in DC activation. (PMID:12902497)
- We have demonstrated the presence of P2Y(14) receptor protein in platelets, but no contribution of this receptor to several measures of platelet function has been observed (PMID:18690346)
- UDP-glucose stimulated IL-8 production via P2RY14 in human endometrial epithelial cells but not stromal cells (PMID:19454705)
- These results support the notion that UDP-glucose is a stable and potent proinflammatory mediator that promotes P2Y(14)-R-mediated neutrophil motility via Rho/Rho kinase activation. (PMID:22673622)
- PPTN as a highly selective high-affinity antagonist of the P2Y14-R. (PMID:23592514)
- UDP-glucose activates P2Y14 receptor and JAK2, increases STAT3 Tyr705 phosphorylation, and enhances transcription of HAS2. (PMID:24847057)
- Data show that thymidine 5’-O-monophosphorothioate (TMPS) diminished UDPG-evoked intracellular calcium mobilization in a stable HEK293T cell line overexpressing the P2Y14 receptor. (PMID:27732965)
- Present study suggests that P2Y14 expression could be used as a phenotypic marker to further dissect placental HSPCs. (PMID:28804125)
- P2Y14R is downregulated in hCPCs derived from heart failure patients. Augmenting P2Y14R expression levels in aged/diseased hCPCs antagonizes senescence and improves functional responses. (PMID:28980705)
- UDP-glucose, a cellular danger signal, and nucleotide receptor P2Y14 enhance the invasion of human extravillous trophoblast cells. (PMID:33011563)
- P2Y14 Receptor as a Target for Neutrophilia Attenuation in Severe COVID-19 Cases: From Hematopoietic Stem Cell Recruitment and Chemotaxis to Thrombo-inflammation. (PMID:33575962)
- The purinergic P2Y14 receptor links hepatocyte death to hepatic stellate cell activation and fibrogenesis in the liver. (PMID:35385339)
- Expression of the pro-inflammatory P2Y14 receptor in the non-vasectomized and vasectomized human epididymis. (PMID:36029226)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | P2RY14 | ENSDARG00000103305 |
| mus_musculus | P2ry14 | ENSMUSG00000036381 |
| rattus_norvegicus | P2ry14 | ENSRNOG00000013872 |
Paralogs (6): GPR87 (ENSG00000138271), P2RY12 (ENSG00000169313), PTAFR (ENSG00000169403), GPR34 (ENSG00000171659), GPR171 (ENSG00000174946), P2RY13 (ENSG00000181631)
Protein
Protein identifiers
P2Y purinoceptor 14 — Q15391 (reviewed: Q15391)
Alternative names: G-protein coupled receptor 105, UDP-glucose receptor
All UniProt accessions (3): Q15391, A5JUU3, C9JAB5
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for UDP-glucose and other UDP-sugar coupled to G-proteins. Not activated by ATP, ADP, UTP or ATP.
Subcellular location. Cell membrane.
Tissue specificity. Highest expression in the placenta, adipose tissue, stomach and intestine, intermediate levels in the brain, spleen, lung and heart, lowest levels in the kidney.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (2): NP_001074924, NP_055694* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR005466 | P2Y14_rcpt | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
Pfam: PF00001
UniProt features (21 total): topological domain 8, transmembrane region 7, glycosylation site 2, chain 1, disulfide bond 1, sequence variant 1, sequence conflict 1
Structure
Experimental structures (PDB)
6 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9J0F | ELECTRON MICROSCOPY | 2.76 |
| 9J0I | ELECTRON MICROSCOPY | 2.76 |
| 9J0B | ELECTRON MICROSCOPY | 2.88 |
| 9YDV | ELECTRON MICROSCOPY | 3.05 |
| 9YDU | ELECTRON MICROSCOPY | 3.19 |
| 9J05 | ELECTRON MICROSCOPY | 3.2 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q15391-F1 | 87.44 | 0.69 |
Antibody-complex structures (SAbDab): 4 — 9J05, 9J0B, 9J0I, 9YDU
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): 94–172
Glycosylation sites (2): 3, 161
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: 279 (showing top):
WALLACE_PROSTATE_CANCER_RACE_UP, GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, MODULE_64, REACTOME_P2Y_RECEPTORS, MODULE_289, WONG_ENDMETRIUM_CANCER_DN, DELYS_THYROID_CANCER_DN, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, MODULE_123, TONKS_TARGETS_OF_RUNX1_RUNX1T1_FUSION_MONOCYTE_DN, WANG_TARGETS_OF_MLL_CBP_FUSION_UP, GOBP_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, GOBP_MULTICELLULAR_ORGANISMAL_LEVEL_HOMEOSTASIS, HOEBEKE_LYMPHOID_STEM_CELL_UP, HESS_TARGETS_OF_HOXA9_AND_MEIS1_DN
GO Biological Process (4): G protein-coupled receptor signaling pathway (GO:0007186), hematopoietic stem cell homeostasis (GO:0061484), signal transduction (GO:0007165), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589)
GO Molecular Function (3): G protein-coupled purinergic nucleotide receptor activity (GO:0045028), G protein-coupled UDP receptor activity (GO:0045029), G protein-coupled receptor activity (GO:0004930)
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 |
| signal transduction | 1 |
| homeostasis of number of cells | 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 |
| G protein-coupled receptor signaling pathway | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
718 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| P2RY14 | P2RX1 | P51575 | 893 |
| P2RY14 | P2RX6 | O15547 | 731 |
| P2RY14 | P2RX5 | Q93086 | 723 |
| P2RY14 | P2RX2 | Q9UBL9 | 715 |
| P2RY14 | P2RX3 | P56373 | 665 |
| P2RY14 | P2RX4 | Q99571 | 635 |
| P2RY14 | ALDH18A1 | P54886 | 577 |
| P2RY14 | P2RY12 | Q9H244 | 546 |
| P2RY14 | P2RX7 | Q99572 | 526 |
| P2RY14 | ENTPD1 | P49961 | 523 |
| P2RY14 | CD38 | P28907 | 492 |
| P2RY14 | ADORA3 | P0DMS8 | 492 |
| P2RY14 | PPBP | P02775 | 491 |
| P2RY14 | P2RY1 | P47900 | 480 |
| P2RY14 | PTGER3 | P43115 | 470 |
IntAct
3 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| P2RY14 | ATP12A | psi-mi:“MI:0915”(physical association) | 0.400 |
BioGRID (6): ATP12A (Affinity Capture-MS), APOB (Affinity Capture-MS), RAP2A (Affinity Capture-MS), ATP12A (Affinity Capture-MS), ATP12A (Affinity Capture-MS), P2RY14 (Affinity Capture-MS)
ESM2 similar proteins: B5X337, D4A4Q2, D4A7K7, O00398, O14626, O35881, P21556, P25105, P32249, P43657, P60019, Q15391, Q1RMI1, Q2NNR5, Q3SAG9, Q3SX17, Q3U507, Q3U6B2, Q3UJF0, Q3ZBK9, Q4G072, Q5ZI82, Q6XCF2, Q80Z39, Q8BFU7, Q8BG55, Q8BLG2, Q8BMC0, Q920A1, Q924T8, Q924T9, Q95KC3, Q95N02, Q95N03, Q99677, Q99JA4, Q99MT7, Q9BXC1, Q9BY21, Q9CPV9
Diamond homologs: D4A4Q2, O14626, O35881, P30992, P32250, Q15391, Q3SX17, Q3ZBK9, Q6GUG4, Q8BG55, Q95KC3, Q99MT7, Q9BE53, Q9BPV8, Q9BY21, Q9CPV9, Q9D8I2, Q9EPX4, Q9ESG6, Q9H244, O00254, P25105, Q28553, P60019, Q05394, Q3SAG9, Q6XCF2, Q9R1K6, Q9UPC5, B0UXR0, C8YUV0, E9QJ73, O02213, O08786, O09047, O16020, O42179, O55197, O57422, O70129
SIGNOR signaling
6 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| P2RY14 | “up-regulates activity” | GNAI1 | binding |
| P2RY14 | “up-regulates activity” | GNAI3 | binding |
| P2RY14 | “up-regulates activity” | GNAO1 | binding |
| P2RY14 | “up-regulates activity” | GNAZ | binding |
| P2RY14 | “up-regulates activity” | GNA14 | binding |
| UDP-D-glucose | “up-regulates activity” | P2RY14 | “chemical activation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
2 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 1 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1090 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:151268942:T:TA | donor_gain | 0.9900 |
| 3:151278281:TCTTA:T | donor_loss | 0.9900 |
| 3:151278282:CTTA:C | donor_loss | 0.9900 |
| 3:151278283:TTA:T | donor_loss | 0.9900 |
| 3:151278284:TA:T | donor_loss | 0.9900 |
| 3:151278285:A:AT | donor_loss | 0.9900 |
| 3:151214341:C:CC | acceptor_gain | 0.9800 |
| 3:151248978:C:CT | acceptor_gain | 0.9800 |
| 3:151248979:A:T | acceptor_gain | 0.9800 |
| 3:151278502:G:GT | donor_gain | 0.9800 |
| 3:151214342:T:G | acceptor_loss | 0.9700 |
| 3:151234707:A:AG | donor_gain | 0.9700 |
| 3:151278286:CCTG:C | donor_gain | 0.9700 |
| 3:151278285:A:AC | donor_gain | 0.9600 |
| 3:151278286:C:CC | donor_gain | 0.9600 |
| 3:151214336:GAGGC:G | acceptor_gain | 0.9500 |
| 3:151214339:GC:G | acceptor_gain | 0.9500 |
| 3:151214340:CC:C | acceptor_gain | 0.9500 |
| 3:151214338:GGC:G | acceptor_gain | 0.9400 |
| 3:151223727:CT:C | donor_gain | 0.9400 |
| 3:151277952:CACAT:C | donor_gain | 0.9400 |
| 3:151214344:AAAAG:A | acceptor_loss | 0.9300 |
| 3:151214345:AAAGA:A | acceptor_loss | 0.9300 |
| 3:151219641:TC:T | acceptor_gain | 0.9300 |
| 3:151219642:CC:C | acceptor_gain | 0.9300 |
| 3:151277960:CGAG:C | donor_gain | 0.9300 |
| 3:151214343:GAAAA:G | acceptor_loss | 0.9200 |
| 3:151220778:T:A | acceptor_gain | 0.9200 |
| 3:151272915:T:G | donor_gain | 0.9200 |
| 3:151219639:GATCC:G | acceptor_loss | 0.9000 |
AlphaMissense
2238 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:151213969:G:C | S116R | 0.997 |
| 3:151213969:G:T | S116R | 0.997 |
| 3:151213971:T:G | S116R | 0.997 |
| 3:151213579:A:C | F246L | 0.994 |
| 3:151213579:A:T | F246L | 0.994 |
| 3:151213581:A:G | F246L | 0.994 |
| 3:151213574:G:C | P248R | 0.993 |
| 3:151213584:A:G | C245R | 0.993 |
| 3:151213881:A:G | W146R | 0.993 |
| 3:151213881:A:T | W146R | 0.993 |
| 3:151214138:A:G | L60P | 0.993 |
| 3:151213574:G:T | P248H | 0.992 |
| 3:151213770:A:G | W183R | 0.992 |
| 3:151213770:A:T | W183R | 0.992 |
| 3:151213452:A:G | C289R | 0.991 |
| 3:151213732:G:C | F195L | 0.991 |
| 3:151213732:G:T | F195L | 0.991 |
| 3:151213734:A:G | F195L | 0.991 |
| 3:151213779:C:G | G180R | 0.991 |
| 3:151213779:C:T | G180R | 0.991 |
| 3:151214036:C:G | C94S | 0.991 |
| 3:151214037:A:T | C94S | 0.991 |
| 3:151213980:C:G | G113R | 0.990 |
| 3:151213980:C:T | G113R | 0.990 |
| 3:151213442:G:C | P292R | 0.989 |
| 3:151213442:G:T | P292H | 0.989 |
| 3:151213790:T:A | K176I | 0.989 |
| 3:151213802:C:G | C172S | 0.989 |
| 3:151213803:A:T | C172S | 0.989 |
| 3:151213993:G:C | S108R | 0.989 |
dbSNP variants (sampled 300 via entrez): RS1000049511 (3:151276390 A>G), RS1000063757 (3:151237579 G>A), RS1000091648 (3:151270171 T>C), RS1000102806 (3:151265184 A>G), RS1000245847 (3:151246811 A>G), RS1000307801 (3:151219233 T>G), RS1000315069 (3:151258027 T>C), RS1000331811 (3:151276463 T>C), RS1000361948 (3:151218763 A>T), RS1000366101 (3:151270084 AGAT>A), RS1000519932 (3:151237330 G>A,T), RS1000550293 (3:151241601 G>A), RS1000602410 (3:151241367 G>A,T), RS1000709801 (3:151247059 G>A,T), RS1000761730 (3:151252324 G>A)
Disease associations
OMIM: gene MIM:610116 | 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 |
|---|---|---|
| GCST006479_120 | Diverticular disease | 9.000000e-11 |
| GCST90002381_192 | Eosinophil count | 1.000000e-09 |
| GCST90002407_414 | White blood cell count | 2.000000e-15 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0009959 | diverticular disease |
| EFO:0004842 | eosinophil count |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4518 (SINGLE PROTEIN), CHEMBL4524011 (PROTEIN FAMILY)
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 (22 total), top 22:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| PPTN | Antagonist | 10.1 | pKi |
| MRS4174 | Antagonist | 10.1 | pKi |
| P2Y14R antagonist I-17 | Antagonist | 9.22 | pIC50 |
| α.β-methylene-2-thio-UDP | Full agonist | 9.04 | pEC50 |
| MRS4183 | Agonist | 9.02 | pEC50 |
| MRS2905 | Agonist | 9.0 | pEC50 |
| 2-thio-UDP | Full agonist | 8.72 | pEC50 |
| MRS4738 | Antagonist | 8.51 | pIC50 |
| MRS4833 | Antagonist | 8.23 | pIC50 |
| MRS4654 | Antagonist | 7.82 | pIC50 |
| compound A [PMID: 40037063] | Antagonist | 7.63 | pIC50 |
| MRS4625 | Antagonist | 7.56 | pIC50 |
| MRS2690 | Agonist | 7.31 | pEC50 |
| UDP-glucuronic acid | Full agonist | 7.2 | pEC50 |
| MRS2802 | Agonist | 7.2 | pEC50 |
| α,β-difluoromethylene-UDP | Agonist | 7.2 | pEC50 |
| UDP | Full agonist | 7.13 | pEC50 |
| UDP-glucose | Full agonist | 7.1 | pIC50 |
| UDP-galactose | Full agonist | 7.0 | pEC50 |
| MRS4458 | Antagonist | 6.77 | pIC50 |
| MRS4478 | Antagonist | 6.57 | pIC50 |
| UDP N-acetyl-glucosamine | Full agonist | 6.0 | pEC50 |
Binding affinities (BindingDB)
7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea | KD | 450 nM |
| N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | KD | 1100 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
| CHEMBL5437512 | IC50 | 25900 nM |
ChEMBL bioactivities
426 potent at pChembl≥5 of 451 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.10 | Ki | 0.08 | nM | CHEMBL4447162 |
| 10.10 | Ki | 0.08 | nM | CHEMBL5271821 |
| 10.10 | Ki | 0.08 | nM | CHEMBL6165236 |
| 9.96 | Kd | 0.11 | nM | CHEMBL5557370 |
| 9.40 | IC50 | 0.4 | nM | PPTN |
| 9.40 | IC50 | 0.4 | nM | CHEMBL5561048 |
| 9.37 | Ki | 0.43 | nM | PPTN |
| 9.30 | IC50 | 0.5 | nM | PPTN |
| 9.30 | IC50 | 0.5 | nM | CHEMBL4743495 |
| 9.26 | IC50 | 0.55 | nM | CHEMBL5568116 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL5557370 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL6169785 |
| 9.08 | IC50 | 0.84 | nM | CHEMBL6163632 |
| 9.04 | EC50 | 0.92 | nM | CHEMBL611791 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5517984 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5537095 |
| 8.89 | IC50 | 1.29 | nM | CHEMBL5561440 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL6164437 |
| 8.82 | IC50 | 1.52 | nM | CHEMBL5561910 |
| 8.75 | IC50 | 1.77 | nM | CHEMBL4436879 |
| 8.72 | IC50 | 1.9 | nM | CHEMBL5558182 |
| 8.72 | EC50 | 1.92 | nM | CHEMBL216011 |
| 8.71 | IC50 | 1.93 | nM | CHEMBL5208130 |
| 8.70 | IC50 | 1.98 | nM | PPTN |
| 8.70 | IC50 | 2 | nM | CHEMBL5186555 |
| 8.70 | IC50 | 2 | nM | PPTN |
| 8.66 | IC50 | 2.18 | nM | CHEMBL4854775 |
| 8.64 | Ki | 2.3 | nM | PPTN |
| 8.64 | Ki | 2.3 | nM | CHEMBL4743495 |
| 8.58 | IC50 | 2.63 | nM | CHEMBL4858280 |
| 8.53 | IC50 | 2.95 | nM | CHEMBL4875670 |
| 8.51 | IC50 | 3.11 | nM | CHEMBL5085823 |
| 8.50 | IC50 | 3.17 | nM | CHEMBL4577585 |
| 8.47 | IC50 | 3.4 | nM | PPTN |
| 8.46 | Ki | 3.44 | nM | CHEMBL5399275 |
| 8.42 | IC50 | 3.83 | nM | CHEMBL5194881 |
| 8.42 | IC50 | 3.81 | nM | CHEMBL5203559 |
| 8.42 | IC50 | 3.8 | nM | CHEMBL5532171 |
| 8.40 | IC50 | 4.01 | nM | CHEMBL5182459 |
| 8.40 | IC50 | 3.97 | nM | CHEMBL5561359 |
| 8.40 | IC50 | 4.01 | nM | CHEMBL5568047 |
| 8.38 | IC50 | 4.16 | nM | CHEMBL5175291 |
| 8.38 | IC50 | 4.2 | nM | CHEMBL5561561 |
| 8.36 | IC50 | 4.35 | nM | CHEMBL4538561 |
| 8.34 | IC50 | 4.54 | nM | CHEMBL4455311 |
| 8.33 | IC50 | 4.66 | nM | CHEMBL5192153 |
| 8.33 | IC50 | 4.65 | nM | CHEMBL5189241 |
| 8.32 | IC50 | 4.8 | nM | CHEMBL5193065 |
| 8.32 | IC50 | 4.83 | nM | CHEMBL5185002 |
| 8.32 | IC50 | 4.8 | nM | PPTN |
PubChem BioAssay actives
382 with measured affinity, of 902 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 |
|---|---|---|---|---|
| 4-[4-[1-[4-[1-[6-[[4-(3-amino-6-imino-4,5-disulfoxanthen-9-yl)-3-carboxybenzoyl]amino]hexyl]triazol-4-yl]butyl]piperidin-4-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1551934: Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assay | ki | 0.0001 | uM |
| N-(3H-benzimidazol-5-yl)-2-(4-bromophenoxy)acetamide | 2078096: Binding affinity to NHS-LC-biotin-labeled P2Y14R (unknown origin) immobilized in SSA sensor assessed as dissociation constant by BLI assay | kd | 0.0001 | uM |
| 4-[4-[1-[4-[1-[6-[[3-acetyl-4-(3-amino-6-imino-4,5-disulfoxanthen-9-yl)benzoyl]amino]hexyl]triazol-4-yl]butyl]piperidin-4-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1953784: Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition constant | ki | 0.0001 | uM |
| 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]thiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0004 | uM |
| 4-(4-piperidin-4-ylphenyl)-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1626550: Antagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method | ic50 | 0.0004 | uM |
| 4-[(4-methylbenzoyl)amino]-5-[(5-methyl-2-pyridinyl)oxy]thiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0006 | uM |
| N,N-diethylethanamine;[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]methylphosphonic acid | 444563: Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production | ec50 | 0.0009 | uM |
| N-(3H-benzimidazol-5-yl)-2-[4-(hydroxymethyl)phenoxy]acetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0011 | uM |
| 4-[(4-methoxybenzoyl)amino]-5-[(6-methyl-3-pyridinyl)oxy]thiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0013 | uM |
| N-(3H-benzimidazol-5-yl)-2-(4-formylphenoxy)acetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0013 | uM |
| 4-[4-[1-[4-[4-[(3’,6’-dihydroxy-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-yl)carbamothioylamino]butanoylamino]butanoyl]piperidin-4-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0015 | uM |
| 3-[(4-methylbenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0018 | uM |
| 1-[(4-fluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0019 | uM |
| [(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methyl phosphono hydrogen phosphate | 444563: Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production | ec50 | 0.0019 | uM |
| N-(3H-benzimidazol-5-yl)-2-(4-chlorophenoxy)acetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0019 | uM |
| N-[3-(1,3-benzoxazol-2-yl)phenyl]-2-(4-methoxyphenyl)acetamide | 1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay | ic50 | 0.0020 | uM |
| 3-(furan-3-yl)-5-[(4-methylbenzoyl)amino]benzoic acid | 1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay | ic50 | 0.0022 | uM |
| 3-[(4-methylbenzoyl)amino]-5-(1H-pyrazol-5-yl)benzoic acid | 1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay | ic50 | 0.0026 | uM |
| 3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(4-methylbenzoyl)amino]benzoic acid | 1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay | ic50 | 0.0029 | uM |
| 4-[4-[(1S,4S,5S)-2-azabicyclo[2.2.1]heptan-5-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1822898: Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis | ic50 | 0.0031 | uM |
| 3-(4-piperidin-4-ylphenyl)-5-(pyridine-4-carbonylamino)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0032 | uM |
| 4-[4-[(1R,5S)-6-hydroxy-3-azabicyclo[3.1.1]heptan-6-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1982180: Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells assessed as inhibition constant by flow cytometry | ki | 0.0034 | uM |
| 5-[(4-methylbenzoyl)amino]-1-[[4-(trifluoromethyl)phenyl]methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0038 | uM |
| 5-[(4-acetylbenzoyl)amino]-1-[(4-fluorophenyl)methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0038 | uM |
| N-(3H-benzimidazol-5-yl)-2-[4-(trifluoromethyl)phenoxy]acetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0038 | uM |
| 5-[(4-methylbenzoyl)amino]-1-[(3,4,5-trifluorophenyl)methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0040 | uM |
| 4-[(4-methylbenzoyl)amino]-5-(4-methylphenoxy)thiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0040 | uM |
| 2-(4-methylphenoxy)-N-quinolin-7-ylacetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0040 | uM |
| 1-[(3,4-difluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0042 | uM |
| 2-(4-methoxyphenoxy)-N-quinolin-7-ylacetamide | 2078095: Antagonist activity at human P2Y14R stably expressed in HEK293 cells assessed as inhibition of forskolin-reduced cAMP production incubated for 30 mins by cAMP-Glo assay | ic50 | 0.0042 | uM |
| 3-(4-piperidin-4-ylphenyl)-5-(pyrazine-2-carbonylamino)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0043 | uM |
| 3-[(4-cyanobenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0045 | uM |
| 5-[(4-ethylbenzoyl)amino]-1-[(4-fluorophenyl)methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0046 | uM |
| 1-[(4-cyanophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0047 | uM |
| N-[3-(1,3-benzoxazol-2-yl)phenyl]-2-[4-(trifluoromethoxy)phenyl]acetamide | 1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay | ic50 | 0.0048 | uM |
| 5-[(4-methylbenzoyl)amino]-1-[[2-(trifluoromethyl)phenyl]methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0048 | uM |
| 3-[(4-methylbenzoyl)amino]-5-phenylbenzoic acid | 1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay | ic50 | 0.0049 | uM |
| 3-benzamido-5-(4-piperidin-4-ylphenyl)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0050 | uM |
| 5-[(4-methylbenzoyl)amino]-1-[(4-nitrophenyl)methyl]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0050 | uM |
| 3-[(4-nitrobenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid | 1564199: Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay | ic50 | 0.0051 | uM |
| 1-[(3-fluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0054 | uM |
| 4-[4-[(3aR,6aR)-5-hydroxy-2,3,3a,4,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-5-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1982180: Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells assessed as inhibition constant by flow cytometry | ki | 0.0055 | uM |
| 4-[4-(azepan-4-yl)phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1982180: Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells assessed as inhibition constant by flow cytometry | ki | 0.0056 | uM |
| 4-[4-(2-azaspiro[3.3]hept-6-en-6-yl)phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid | 1982180: Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells assessed as inhibition constant by flow cytometry | ki | 0.0056 | uM |
| 1-[(3,5-dimethylphenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0058 | uM |
| N-[3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-2-[4-(trifluoromethyl)phenyl]acetamide | 1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay | ic50 | 0.0061 | uM |
| 4-[(4-methylbenzoyl)amino]-5-(4-methylphenyl)sulfanylthiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0065 | uM |
| 4-[(4-methylbenzoyl)amino]-5-[(6-methyl-3-pyridinyl)oxy]thiophene-2-carboxylic acid | 2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assay | ic50 | 0.0065 | uM |
| N-[3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-2-(4-methylphenyl)acetamide | 1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay | ic50 | 0.0067 | uM |
| 1-[(4-chlorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid | 1896866: Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay | ic50 | 0.0071 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Progesterone | affects cotreatment, increases expression | 3 |
| Estradiol | affects cotreatment, increases expression | 2 |
| Tretinoin | increases expression | 2 |
| triphenyl phosphate | affects expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects response to substance, increases expression, affects cotreatment, decreases expression | 1 |
| tamibarotene | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Allergens | increases expression | 1 |
| Cadmium | decreases expression, increases abundance | 1 |
| Lipopolysaccharides | increases expression, affects cotreatment, decreases expression, affects response to substance | 1 |
| Ozone | increases abundance, affects expression | 1 |
| Valproic Acid | decreases methylation | 1 |
| Mifepristone | increases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
| Cadmium Chloride | decreases expression, increases abundance | 1 |
ChEMBL screening assays
101 unique, capped per target: 58 binding, 43 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1045264 | Functional | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production | Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5’-diphosphoglucose and its replacement with alkyl and aryl groups. — J Med Chem |
| CHEMBL2339544 | Binding | Inhibition of human P2Y14 receptor | Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists. — J Med Chem |
Cellosaurus cell lines
2 cell lines: 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_ZD97 | 1321N1-HA-P2Y14 | Cancer cell line | Male |
| CVCL_ZK28 | T-REx Tango P2RY14-bla U2OS | Cancer cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Galactose