P2RY14

gene
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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

FieldValue
HGNC IDHGNC:16442
Approved symbolP2RY14
Namepurinergic receptor P2Y14
Location3q25.1
Locus typegene with protein product
StatusApproved
AliasesKIAA0001
Ensembl geneENSG00000174944
Ensembl biotypeprotein_coding
OMIM610116
Entrez9934

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

ExonStartEnd
ENSE00001208977151219535151219642
ENSE00001208984151278287151278542
ENSE00001208990151212117151214340

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 IDTPM avgSamples expressed
451350.8704123
451390.4166152
451360.291392
451280.045921
451310.041816
451300.035021
451290.030319
451400.02058
451330.020210
451320.00963

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
deciduaUBERON:000245097.33gold quality
skin of hipUBERON:000155490.51gold quality
endothelial cellCL:000011589.95gold quality
synovial jointUBERON:000221789.89gold quality
upper leg skinUBERON:000426289.45gold quality
calcaneal tendonUBERON:000370187.51gold quality
endometriumUBERON:000129587.03gold quality
mucosa of stomachUBERON:000119985.70gold quality
colonic epitheliumUBERON:000039783.42gold quality
visceral pleuraUBERON:000240182.96gold quality
placentaUBERON:000198782.88gold quality
upper arm skinUBERON:000426382.77gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047382.75gold quality
caecumUBERON:000115382.42gold quality
right lungUBERON:000216782.42gold quality
buccal mucosa cellCL:000233682.36gold quality
rectumUBERON:000105281.90gold quality
vermiform appendixUBERON:000115481.70gold quality
fundus of stomachUBERON:000116080.47gold quality
pleuraUBERON:000097780.38gold quality
dorsal root ganglionUBERON:000004480.33gold quality
mammalian vulvaUBERON:000099779.90gold quality
superficial temporal arteryUBERON:000161479.80silver quality
cardia of stomachUBERON:000116279.47gold quality
mucosa of sigmoid colonUBERON:000499379.30gold quality
oral cavityUBERON:000016779.26gold quality
lower lobe of lungUBERON:000894979.16gold quality
parietal pleuraUBERON:000240078.77gold quality
transverse colonUBERON:000115778.27gold quality
body of stomachUBERON:000116178.10gold quality

Single-cell (SCXA)

Detected in 7 experiment(s), a significant marker in 7.

ExperimentMarker?Max mean expression
E-HCAD-25yes462.46
E-MTAB-6701yes115.20
E-MTAB-8498yes13.50
E-CURD-112yes12.70
E-HCAD-11yes9.14
E-MTAB-9801yes6.78
E-ANND-3yes4.09

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):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-6833-3P100.0070.633197
HSA-MIR-432-3P100.0067.86705
HSA-MIR-4768-5P100.0069.492861
HSA-MIR-34A-5P99.9971.211784
HSA-MIR-449A99.9971.051776
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-186-5P99.9970.833707
HSA-MIR-477599.9875.006394
HSA-MIR-34C-5P99.9770.451577
HSA-MIR-449B-5P99.9770.261580
HSA-MIR-50799.9770.111915
HSA-MIR-570-3P99.9672.414910
HSA-MIR-302E99.9670.742669
HSA-MIR-4666A-3P99.9671.713434
HSA-MIR-55799.9670.011640
HSA-MIR-990299.8969.152250
HSA-MIR-380-3P99.8970.181978
HSA-MIR-302A-3P99.8971.231777
HSA-MIR-302B-3P99.8971.231777
HSA-MIR-302C-3P99.8971.201778
HSA-MIR-302D-3P99.8971.251777
HSA-MIR-373-3P99.8470.681668
HSA-MIR-520E-3P99.8470.551698
HSA-MIR-372-3P99.8370.581691
HSA-MIR-520A-3P99.8370.591687
HSA-MIR-520B-3P99.8370.561699
HSA-MIR-520C-3P99.8370.561699
HSA-MIR-520D-3P99.8370.781676
HSA-MIR-3180-5P99.8269.122422
HSA-MIR-430799.8270.453374

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

OrganismSymbolGene ID
danio_rerioP2RY14ENSDARG00000103305
mus_musculusP2ry14ENSMUSG00000036381
rattus_norvegicusP2ry14ENSRNOG00000013872

Paralogs (6): GPR87 (ENSG00000138271), P2RY12 (ENSG00000169313), PTAFR (ENSG00000169403), GPR34 (ENSG00000171659), GPR171 (ENSG00000174946), P2RY13 (ENSG00000181631)

Protein

Protein identifiers

P2Y purinoceptor 14Q15391 (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)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR005466P2Y14_rcptFamily
IPR017452GPCR_Rhodpsn_7TMDomain

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.

PDBMethodResolution (Å)
9J0FELECTRON MICROSCOPY2.76
9J0IELECTRON MICROSCOPY2.76
9J0BELECTRON MICROSCOPY2.88
9YDVELECTRON MICROSCOPY3.05
9YDUELECTRON MICROSCOPY3.19
9J05ELECTRON MICROSCOPY3.2

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q15391-F187.440.69

Antibody-complex structures (SAbDab): 49J05, 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

IDPathway
R-HSA-417957P2Y receptors
R-HSA-418594G 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:

CategoryPathways
Nucleotide-like (purinergic) receptors1
GPCR downstream signalling1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
G protein-coupled receptor activity2
signal transduction1
homeostasis of number of cells1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
purinergic nucleotide receptor signaling pathway1
purinergic nucleotide receptor activity1
G protein-coupled purinergic nucleotide receptor signaling pathway1
G protein-coupled pyrimidinergic nucleotide receptor activity1
transmembrane signaling receptor activity1
G protein-coupled receptor signaling pathway1
membrane1
cell periphery1
cellular anatomical structure1

Protein interactions and networks

STRING

718 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
P2RY14P2RX1P51575893
P2RY14P2RX6O15547731
P2RY14P2RX5Q93086723
P2RY14P2RX2Q9UBL9715
P2RY14P2RX3P56373665
P2RY14P2RX4Q99571635
P2RY14ALDH18A1P54886577
P2RY14P2RY12Q9H244546
P2RY14P2RX7Q99572526
P2RY14ENTPD1P49961523
P2RY14CD38P28907492
P2RY14ADORA3P0DMS8492
P2RY14PPBPP02775491
P2RY14P2RY1P47900480
P2RY14PTGER3P43115470

IntAct

3 interactions, top by confidence:

ABTypeScore
P2RY14ATP12Apsi-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.

AEffectBMechanism
P2RY14“up-regulates activity”GNAI1binding
P2RY14“up-regulates activity”GNAI3binding
P2RY14“up-regulates activity”GNAO1binding
P2RY14“up-regulates activity”GNAZbinding
P2RY14“up-regulates activity”GNA14binding
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):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance1
Likely benign1
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1090 predictions. Top by Δscore:

VariantEffectΔscore
3:151268942:T:TAdonor_gain0.9900
3:151278281:TCTTA:Tdonor_loss0.9900
3:151278282:CTTA:Cdonor_loss0.9900
3:151278283:TTA:Tdonor_loss0.9900
3:151278284:TA:Tdonor_loss0.9900
3:151278285:A:ATdonor_loss0.9900
3:151214341:C:CCacceptor_gain0.9800
3:151248978:C:CTacceptor_gain0.9800
3:151248979:A:Tacceptor_gain0.9800
3:151278502:G:GTdonor_gain0.9800
3:151214342:T:Gacceptor_loss0.9700
3:151234707:A:AGdonor_gain0.9700
3:151278286:CCTG:Cdonor_gain0.9700
3:151278285:A:ACdonor_gain0.9600
3:151278286:C:CCdonor_gain0.9600
3:151214336:GAGGC:Gacceptor_gain0.9500
3:151214339:GC:Gacceptor_gain0.9500
3:151214340:CC:Cacceptor_gain0.9500
3:151214338:GGC:Gacceptor_gain0.9400
3:151223727:CT:Cdonor_gain0.9400
3:151277952:CACAT:Cdonor_gain0.9400
3:151214344:AAAAG:Aacceptor_loss0.9300
3:151214345:AAAGA:Aacceptor_loss0.9300
3:151219641:TC:Tacceptor_gain0.9300
3:151219642:CC:Cacceptor_gain0.9300
3:151277960:CGAG:Cdonor_gain0.9300
3:151214343:GAAAA:Gacceptor_loss0.9200
3:151220778:T:Aacceptor_gain0.9200
3:151272915:T:Gdonor_gain0.9200
3:151219639:GATCC:Gacceptor_loss0.9000

AlphaMissense

2238 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
3:151213969:G:CS116R0.997
3:151213969:G:TS116R0.997
3:151213971:T:GS116R0.997
3:151213579:A:CF246L0.994
3:151213579:A:TF246L0.994
3:151213581:A:GF246L0.994
3:151213574:G:CP248R0.993
3:151213584:A:GC245R0.993
3:151213881:A:GW146R0.993
3:151213881:A:TW146R0.993
3:151214138:A:GL60P0.993
3:151213574:G:TP248H0.992
3:151213770:A:GW183R0.992
3:151213770:A:TW183R0.992
3:151213452:A:GC289R0.991
3:151213732:G:CF195L0.991
3:151213732:G:TF195L0.991
3:151213734:A:GF195L0.991
3:151213779:C:GG180R0.991
3:151213779:C:TG180R0.991
3:151214036:C:GC94S0.991
3:151214037:A:TC94S0.991
3:151213980:C:GG113R0.990
3:151213980:C:TG113R0.990
3:151213442:G:CP292R0.989
3:151213442:G:TP292H0.989
3:151213790:T:AK176I0.989
3:151213802:C:GC172S0.989
3:151213803:A:TC172S0.989
3:151213993:G:CS108R0.989

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):

StudyTraitp-value
GCST006479_120Diverticular disease9.000000e-11
GCST90002381_192Eosinophil count1.000000e-09
GCST90002407_414White blood cell count2.000000e-15

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0009959diverticular disease
EFO:0004842eosinophil 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:

LigandActionAffinityParameter
PPTNAntagonist10.1pKi
MRS4174Antagonist10.1pKi
P2Y14R antagonist I-17Antagonist9.22pIC50
α.β-methylene-2-thio-UDPFull agonist9.04pEC50
MRS4183Agonist9.02pEC50
MRS2905Agonist9.0pEC50
2-thio-UDPFull agonist8.72pEC50
MRS4738Antagonist8.51pIC50
MRS4833Antagonist8.23pIC50
MRS4654Antagonist7.82pIC50
compound A [PMID: 40037063]Antagonist7.63pIC50
MRS4625Antagonist7.56pIC50
MRS2690Agonist7.31pEC50
UDP-glucuronic acidFull agonist7.2pEC50
MRS2802Agonist7.2pEC50
α,β-difluoromethylene-UDPAgonist7.2pEC50
UDPFull agonist7.13pEC50
UDP-glucoseFull agonist7.1pIC50
UDP-galactoseFull agonist7.0pEC50
MRS4458Antagonist6.77pIC50
MRS4478Antagonist6.57pIC50
UDP N-acetyl-glucosamineFull agonist6.0pEC50

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.

LigandMeasureValue
StaurosporineKD1.7 nM
1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)ureaKD450 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamideKD1100 nM
1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]ureaKD1400 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-carboxamideKD2600 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-carboxamideKD3500 nM
CHEMBL5437512IC5025900 nM

ChEMBL bioactivities

426 potent at pChembl≥5 of 451 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.10Ki0.08nMCHEMBL4447162
10.10Ki0.08nMCHEMBL5271821
10.10Ki0.08nMCHEMBL6165236
9.96Kd0.11nMCHEMBL5557370
9.40IC500.4nMPPTN
9.40IC500.4nMCHEMBL5561048
9.37Ki0.43nMPPTN
9.30IC500.5nMPPTN
9.30IC500.5nMCHEMBL4743495
9.26IC500.55nMCHEMBL5568116
9.22IC500.6nMCHEMBL5557370
9.15IC500.7nMCHEMBL6169785
9.08IC500.84nMCHEMBL6163632
9.04EC500.92nMCHEMBL611791
8.96IC501.1nMCHEMBL5517984
8.89IC501.3nMCHEMBL5537095
8.89IC501.29nMCHEMBL5561440
8.89IC501.3nMCHEMBL6164437
8.82IC501.52nMCHEMBL5561910
8.75IC501.77nMCHEMBL4436879
8.72IC501.9nMCHEMBL5558182
8.72EC501.92nMCHEMBL216011
8.71IC501.93nMCHEMBL5208130
8.70IC501.98nMPPTN
8.70IC502nMCHEMBL5186555
8.70IC502nMPPTN
8.66IC502.18nMCHEMBL4854775
8.64Ki2.3nMPPTN
8.64Ki2.3nMCHEMBL4743495
8.58IC502.63nMCHEMBL4858280
8.53IC502.95nMCHEMBL4875670
8.51IC503.11nMCHEMBL5085823
8.50IC503.17nMCHEMBL4577585
8.47IC503.4nMPPTN
8.46Ki3.44nMCHEMBL5399275
8.42IC503.83nMCHEMBL5194881
8.42IC503.81nMCHEMBL5203559
8.42IC503.8nMCHEMBL5532171
8.40IC504.01nMCHEMBL5182459
8.40IC503.97nMCHEMBL5561359
8.40IC504.01nMCHEMBL5568047
8.38IC504.16nMCHEMBL5175291
8.38IC504.2nMCHEMBL5561561
8.36IC504.35nMCHEMBL4538561
8.34IC504.54nMCHEMBL4455311
8.33IC504.66nMCHEMBL5192153
8.33IC504.65nMCHEMBL5189241
8.32IC504.8nMCHEMBL5193065
8.32IC504.83nMCHEMBL5185002
8.32IC504.8nMPPTN

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.

CompoundAssayTypeValueUnit
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 acid1551934: Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assayki0.0001uM
N-(3H-benzimidazol-5-yl)-2-(4-bromophenoxy)acetamide2078096: Binding affinity to NHS-LC-biotin-labeled P2Y14R (unknown origin) immobilized in SSA sensor assessed as dissociation constant by BLI assaykd0.0001uM
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 acid1953784: Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition constantki0.0001uM
5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]thiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0004uM
4-(4-piperidin-4-ylphenyl)-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid1626550: 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 methodic500.0004uM
4-[(4-methylbenzoyl)amino]-5-[(5-methyl-2-pyridinyl)oxy]thiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0006uM
N,N-diethylethanamine;[[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]methylphosphonic acid444563: 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 productionec500.0009uM
N-(3H-benzimidazol-5-yl)-2-[4-(hydroxymethyl)phenoxy]acetamide2078095: 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 assayic500.0011uM
4-[(4-methoxybenzoyl)amino]-5-[(6-methyl-3-pyridinyl)oxy]thiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0013uM
N-(3H-benzimidazol-5-yl)-2-(4-formylphenoxy)acetamide2078095: 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 assayic500.0013uM
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 acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0015uM
3-[(4-methylbenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid1564199: 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 immunoassayic500.0018uM
1-[(4-fluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0019uM
[(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methyl phosphono hydrogen phosphate444563: 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 productionec500.0019uM
N-(3H-benzimidazol-5-yl)-2-(4-chlorophenoxy)acetamide2078095: 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 assayic500.0019uM
N-[3-(1,3-benzoxazol-2-yl)phenyl]-2-(4-methoxyphenyl)acetamide1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayic500.0020uM
3-(furan-3-yl)-5-[(4-methylbenzoyl)amino]benzoic acid1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayic500.0022uM
3-[(4-methylbenzoyl)amino]-5-(1H-pyrazol-5-yl)benzoic acid1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayic500.0026uM
3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(4-methylbenzoyl)amino]benzoic acid1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayic500.0029uM
4-[4-[(1S,4S,5S)-2-azabicyclo[2.2.1]heptan-5-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid1822898: 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 analysisic500.0031uM
3-(4-piperidin-4-ylphenyl)-5-(pyridine-4-carbonylamino)benzoic acid1564199: 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 immunoassayic500.0032uM
4-[4-[(1R,5S)-6-hydroxy-3-azabicyclo[3.1.1]heptan-6-yl]phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid1982180: 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 cytometryki0.0034uM
5-[(4-methylbenzoyl)amino]-1-[[4-(trifluoromethyl)phenyl]methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0038uM
5-[(4-acetylbenzoyl)amino]-1-[(4-fluorophenyl)methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0038uM
N-(3H-benzimidazol-5-yl)-2-[4-(trifluoromethyl)phenoxy]acetamide2078095: 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 assayic500.0038uM
5-[(4-methylbenzoyl)amino]-1-[(3,4,5-trifluorophenyl)methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0040uM
4-[(4-methylbenzoyl)amino]-5-(4-methylphenoxy)thiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0040uM
2-(4-methylphenoxy)-N-quinolin-7-ylacetamide2078095: 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 assayic500.0040uM
1-[(3,4-difluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0042uM
2-(4-methoxyphenoxy)-N-quinolin-7-ylacetamide2078095: 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 assayic500.0042uM
3-(4-piperidin-4-ylphenyl)-5-(pyrazine-2-carbonylamino)benzoic acid1564199: 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 immunoassayic500.0043uM
3-[(4-cyanobenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid1564199: 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 immunoassayic500.0045uM
5-[(4-ethylbenzoyl)amino]-1-[(4-fluorophenyl)methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0046uM
1-[(4-cyanophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0047uM
N-[3-(1,3-benzoxazol-2-yl)phenyl]-2-[4-(trifluoromethoxy)phenyl]acetamide1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayic500.0048uM
5-[(4-methylbenzoyl)amino]-1-[[2-(trifluoromethyl)phenyl]methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0048uM
3-[(4-methylbenzoyl)amino]-5-phenylbenzoic acid1757151: Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayic500.0049uM
3-benzamido-5-(4-piperidin-4-ylphenyl)benzoic acid1564199: 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 immunoassayic500.0050uM
5-[(4-methylbenzoyl)amino]-1-[(4-nitrophenyl)methyl]pyrazole-3-carboxylic acid1896866: 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 assayic500.0050uM
3-[(4-nitrobenzoyl)amino]-5-(4-piperidin-4-ylphenyl)benzoic acid1564199: 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 immunoassayic500.0051uM
1-[(3-fluorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0054uM
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 acid1982180: 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 cytometryki0.0055uM
4-[4-(azepan-4-yl)phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid1982180: 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 cytometryki0.0056uM
4-[4-(2-azaspiro[3.3]hept-6-en-6-yl)phenyl]-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid1982180: 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 cytometryki0.0056uM
1-[(3,5-dimethylphenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0058uM
N-[3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-2-[4-(trifluoromethyl)phenyl]acetamide1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayic500.0061uM
4-[(4-methylbenzoyl)amino]-5-(4-methylphenyl)sulfanylthiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0065uM
4-[(4-methylbenzoyl)amino]-5-[(6-methyl-3-pyridinyl)oxy]thiophene-2-carboxylic acid2085539: Antagonist activity at P2Y14R (unknown origin) stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP-Glo assayic500.0065uM
N-[3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-2-(4-methylphenyl)acetamide1876617: Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayic500.0067uM
1-[(4-chlorophenyl)methyl]-5-[(4-methylbenzoyl)amino]pyrazole-3-carboxylic acid1896866: 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 assayic500.0071uM

CTD chemical–gene interactions

16 total (human), top 16 by PubMed support.

ChemicalActions (top 5)PubMed papers
Progesteroneaffects cotreatment, increases expression3
Estradiolaffects cotreatment, increases expression2
Tretinoinincreases expression2
triphenyl phosphateaffects expression1
S-(1,2-dichlorovinyl)cysteineaffects response to substance, increases expression, affects cotreatment, decreases expression1
tamibaroteneincreases expression1
di-n-butylphosphoric acidaffects expression1
Air Pollutantsaffects expression, increases abundance1
Allergensincreases expression1
Cadmiumdecreases expression, increases abundance1
Lipopolysaccharidesincreases expression, affects cotreatment, decreases expression, affects response to substance1
Ozoneincreases abundance, affects expression1
Valproic Aciddecreases methylation1
Mifepristoneincreases expression1
Aflatoxin B1increases methylation1
Cadmium Chloridedecreases expression, increases abundance1

ChEMBL screening assays

101 unique, capped per target: 58 binding, 43 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1045264FunctionalAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionHuman P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5’-diphosphoglucose and its replacement with alkyl and aryl groups. — J Med Chem
CHEMBL2339544BindingInhibition of human P2Y14 receptorDiscovery 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):

CellosaurusNameCategorySex
CVCL_ZD971321N1-HA-P2Y14Cancer cell lineMale
CVCL_ZK28T-REx Tango P2RY14-bla U2OSCancer cell lineFemale

Clinical trials (associated diseases)

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