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PTGDR

gene
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Also known as DPDP1PTGDR1

Summary

PTGDR (prostaglandin D2 receptor, HGNC:9591) is a protein-coding gene on chromosome 14q22.1, encoding Prostaglandin D2 receptor (Q13258). Receptor for prostaglandin D2 (PGD2).

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. The receptors are seven-pass transmembrane proteins that respond to extracellular cues and activate intracellular signal transduction pathways. This protein is reported to be a receptor for prostaglandin D2, which is a mediator of allergic inflammation and allergic airway inflammation in asthma. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 5729 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): asthma-related traits, susceptibility to, 1 (Limited, GenCC)
  • Clinical variants (ClinVar): 64 total
  • Druggable target: yes — 14 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_000953

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9591
Approved symbolPTGDR
Nameprostaglandin D2 receptor
Location14q22.1
Locus typegene with protein product
StatusApproved
AliasesDP, DP1, PTGDR1
Ensembl geneENSG00000168229
Ensembl biotypeprotein_coding
OMIM604687
Entrez5729

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000306051, ENST00000553372

RefSeq mRNA: 2 — MANE Select: NM_000953 NM_000953, NM_001281469

CCDS: CCDS61454, CCDS9707

Canonical transcript exons

ENST00000306051 — 2 exons

ExonStartEnd
ENSE000011478585226769852268660
ENSE000013164635227473152276724

Expression profiles

Bgee: expression breadth ubiquitous, 169 present calls, max score 85.77.

FANTOM5 (CAGE): breadth broad, TPM avg 1.1378 / max 159.8544, expressed in 249 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter IDTPM avgSamples expressed
1396040.9173206
1396030.220590

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
granulocyteCL:000009485.77gold quality
mucosa of transverse colonUBERON:000499180.81gold quality
rectumUBERON:000105278.70gold quality
parietal pleuraUBERON:000240078.24gold quality
mucosa of sigmoid colonUBERON:000499377.79gold quality
colonic mucosaUBERON:000031776.31gold quality
germinal epithelium of ovaryUBERON:000130476.21silver quality
trigeminal ganglionUBERON:000167575.95gold quality
bloodUBERON:000017875.64gold quality
pleuraUBERON:000097775.20gold quality
transverse colonUBERON:000115773.25gold quality
spleenUBERON:000210672.91gold quality
visceral pleuraUBERON:000240172.88gold quality
apex of heartUBERON:000209871.93gold quality
calcaneal tendonUBERON:000370171.24gold quality
colonic epitheliumUBERON:000039769.61silver quality
right coronary arteryUBERON:000162567.37gold quality
lymph nodeUBERON:000002966.95gold quality
subcutaneous adipose tissueUBERON:000219066.05gold quality
colonUBERON:000115566.04gold quality
large intestineUBERON:000005966.03gold quality
superficial temporal arteryUBERON:000161465.78silver quality
gall bladderUBERON:000211065.48gold quality
tibial nerveUBERON:000132364.79gold quality
caecumUBERON:000115364.26gold quality
leukocyteCL:000073864.25gold quality
vermiform appendixUBERON:000115463.82gold quality
amniotic fluidUBERON:000017363.75silver quality
intestineUBERON:000016063.60gold quality
heart left ventricleUBERON:000208463.46gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-HCAD-30yes832.60
E-CURD-122yes32.70
E-ANND-3yes13.62
E-MTAB-6678yes10.21

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ATF7, HR, NFKB, PEG3, TBX1, TP53

miRNA regulators (miRDB)

85 targeting PTGDR, 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-3163100.0077.238605
HSA-MIR-3646100.0073.565283
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-656-3P100.0072.152788
HSA-MIR-366299.9973.825684
HSA-MIR-186-5P99.9970.833707
HSA-MIR-428299.9975.366408
HSA-MIR-27A-3P99.9872.132955
HSA-MIR-27B-3P99.9872.132955
HSA-MIR-998599.9872.112939
HSA-MIR-499A-5P99.9870.791323
HSA-MIR-314899.9775.066478
HSA-MIR-60799.9773.625593
HSA-MIR-548AT-5P99.9670.832666
HSA-MIR-548AJ-3P99.9673.385345
HSA-MIR-548X-3P99.9673.385345
HSA-MIR-335-3P99.9373.364958
HSA-MIR-338-5P99.9272.342951
HSA-MIR-808799.9069.551351
HSA-MIR-3140-3P99.8868.472069
HSA-MIR-7845-5P99.8864.88771
HSA-MIR-106B-5P99.8874.722795
HSA-MIR-20A-5P99.8874.762769
HSA-MIR-182-5P99.8774.032589
HSA-MIR-684499.8270.692423
HSA-MIR-205299.7969.372031
HSA-MIR-7856-5P99.7569.992901
HSA-MIR-6885-3P99.7570.363187
HSA-MIR-4446-5P99.7269.192544

Literature-anchored findings (GeneRIF, showing 40)

  • New polymorphisms of human prostanoid DP receptor gene. (PMID:12002745)
  • Association of a new-type prostaglandin D2 receptor CRTH2 with circulating T helper 2 cells in patients with atopic dermatitis. (PMID:12230502)
  • amino acid sequence alignment of human, mouse and rat DP receptors (PMID:12895603)
  • Activation of the D prostanoid receptor DP1 impedes the TNF-alpha-induced migration of Langerhans cells (LC) from skin explants and strongly inhibits chemotactic responses of LC precursors and maturing LCs to CC chemokine ligands 20 and 19, respectively. (PMID:15004188)
  • Our functional and genetic findings identify PTGDR as an asthma-susceptibility gene. (PMID:15496624)
  • DP2 might play a critical role in allergic diseases (PMID:15749909)
  • activation of the prostanoid DP receptor on THP-1 cells enhances TNF-alpha-induced MCP-1 and IL-8 production via the cAMP/PKA signaling pathway (PMID:17307163)
  • study demonstrated significant evidence of association between polymorphisms in PTGDR with asthma phenotypes in two Caucasian populations (PMID:17538632)
  • Review. PGD(2) exerts its effects partly through the D-prostanoid receptor. The distribution of DP expression depends on the type of tissue and environment with/without inflammation. (PMID:17541272)
  • These results suggest that the three PTGDR gene promoter polymorphisms studied are not important risk factors for asthma susceptibility in the Chinese Han population. (PMID:17845306)
  • D-type prostanoid (DP) receptors comediate with CRTH2 the mobilization of eosinophils from bone marrow and their chemotaxis, which might provide the rationale for DP antagonists in the treatment of allergic disease (PMID:17878378)
  • activation of DP(1) may contribute to the long lasting blood flow changes in the target organ–REVIEW (PMID:17965752)
  • Expression of prostaglandin E(2) receptors (EP(2), EP(3), EP(4)), prostaglandin D(2) receptor (DP(2)), prostanoid thromboxane A(2) receptor (TP) and to a lesser extent EP(1) were observed in several hair follicle compartments. (PMID:18005048)
  • level of exptression in nasal polyps correlates with chronic rhinosinusitis associated with bronchial asthma (PMID:18797183)
  • These results suggest that expression of DP and CRTH2 is associated with the pathophysiology of chronic rhinosinusitis, and the expression of these receptors may be regulated by h-PGDS and PGD. (PMID:18802357)
  • promoter polymorphism association in Spanish children with asthma (PMID:18811623)
  • PGD(2) induces HO-1 mRNA expression through DP2 receptor, linking the PGD(2)-DP2 signaling with heme homeostasis. (PMID:18957281)
  • Our results do not support PTGDR to be a major candidate gene for asthma traits and atopy in Chinese children. (PMID:19220773)
  • Prostanoid DP receptor (PTGDR) polymorhisms variants was found in a subset of mothers with post-coital associated preterm births (PMID:19710676)
  • Mast cell-derived prostaglandin D2 controls hyaluronan synthesis in human orbital fibroblasts via DP1 activation: implications for thyroid eye disease. (PMID:20308056)
  • during allergen-elicited eosinophilic inflammatory reactions, cysteinyl-leukotriene production is regulated by DP1/DP2-orchestrated eosinophil activation (PMID:20973774)
  • These results suggest that despite the non-significant findings in the present study populations, prostanoid D2 receptor promoter haplotypes may account for a small but significant proportion of the risk of asthma in Caucasian populations. (PMID:21199159)
  • Polymorphisms of the PTGDR and LTC4S influence responsiveness to leukotriene receptor antagonists in Korean children with asthma. (PMID:21307858)
  • DP(1) receptors coupled to G(alphas) increase adenylate cyclase activity and cAMP/protein kinase A-dependent formation of lipid bodies, and DP(2) receptors coupled to G(alphai) increase calcium; each of these signals is required for LTC(4) production (PMID:21426314)
  • DP mediates eosinophils through the elevation of intracellular cAMP production but does not change CRTH2 expression; balance between DP and CRTH2 could influence the degree of PGD2-induced eosinophil migration (PMID:21624751)
  • PGD(2) can induce MUC5B overproduction via ERK MAPK/RSK1/CREB signaling and that DP1 receptor may have suppressive effects in controlling MUC5B overproduction in the airway. (PMID:21832046)
  • Genetic combinations described have functional implications in the PTGDR promoter activity by changing the transcription factors affinity that will help characterize different risk groups. (PMID:21883277)
  • DP receptors amplify the biological response to CRTH2 activation and the CRTH2/DP heteromer might represent both a functional signaling unit for PGD(2) and a potential target for development of heteromer-directed therapy for allergic diseases (PMID:21930295)
  • The PTGDR -441C/T polymorphism is not associated with asthma or its phenotypes in the North Indian population. (PMID:22182808)
  • Genetic variant may play a role in NSAID induced acute urticaria. (PMID:23181793)
  • the PTGDR -549 C/T polymorphism confers susceptibility to asthma in Europeans and adults. However, no association was found between the PTGDR 441 C/T and -197 C/T polymorphisms or the CCC and TCT haplotypes and asthma susceptibility. (PMID:23192614)
  • PGD(2)-DP signaling reduces vascular permeability via endothelial cAMP/PKA/Tiam1/Rac1 pathway. (PMID:23307871)
  • Lipocalin-type prostaglandin D2 (PGD2) synthase (L-PGDS) interacts intracellularly with the G protein-coupled receptor DP1 in an agonist-independent manner. (PMID:24493589)
  • Low DP1 prostanoid receptor is associated with gastric cancer progression. (PMID:24922638)
  • Non-obligatory role of prostaglandin D2 receptor subtype 1 in rosacea: laropiprant in comparison to a placebo did not alleviate the symptoms of erythematoelangiectaic rosacea (PMID:25142778)
  • EP2 receptors exhibit more constraints to mutations than DP receptors. (PMID:25681680)
  • PGD2 markedly augments disease activity through its ability to enhance the proinflammatory actions of macrophages and subsequent neutrophil activation. (PMID:26792210)
  • An association was found between single nucleotide polymorphisms of the PTGFR and SLCO2A1 genes and the response to latanoprost in Han Chinese patients with glaucoma. These SNPs may be important determinants of differential response to latanoprost. (PMID:27336732)
  • EP2 receptors seem to be able to distinguish endogenous ligands PGD2, PGE2 or prostaglandin F2alpha better than DP receptors. (PMID:27636113)
  • PGD2 signaling through the D-prostanoid receptor 1 (DP1) receptor is necessary for optimal microglia/macrophage activation and IFN expression after infection with a neurotropic coronavirus (PMID:28630327)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
mus_musculusPtgdrENSMUSG00000071489
rattus_norvegicusPtgdrENSRNOG00000031307
rattus_norvegicusPtgdrl1ENSRNOG00000031535

Paralogs (7): TBXA2R (ENSG00000006638), PTGER3 (ENSG00000050628), PTGFR (ENSG00000122420), PTGER2 (ENSG00000125384), PTGIR (ENSG00000160013), PTGER1 (ENSG00000160951), PTGER4 (ENSG00000171522)

Protein

Protein identifiers

Prostaglandin D2 receptor — Q13258 (reviewed: Q13258)

Alternative names: Prostanoid DP receptor

All UniProt accessions (1): Q13258

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for prostaglandin D2 (PGD2). The activity of this receptor is mainly mediated by G(s) proteins that stimulate adenylate cyclase, resulting in an elevation of intracellular cAMP. A mobilization of calcium is also observed, but without formation of inositol 1,4,5-trisphosphate. Involved in PLA2G3-dependent maturation of mast cells. PLA2G3 is secreted by immature mast cells and acts on nearby fibroblasts upstream to PTDGS to synthesize PGD2, which in turn promotes mast cell maturation and degranulation via PTGDR.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in retinal choroid, ciliary epithelium, longitudinal and circular ciliary muscles, iris, small intestine and platelet membranes.

Disease relevance. Asthma-related traits 1 (ASRT1) [MIM:607277] Asthma-related traits include clinical symptoms of asthma, such as coughing, wheezing, dyspnea, bronchial hyperresponsiveness as assessed by methacholine challenge test, serum IgE levels, atopy and atopic dermatitis. Disease susceptibility is associated with variants affecting the gene represented in this entry.

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

Isoforms (2)

UniProt IDNamesCanonical?
Q13258-11yes
Q13258-22

RefSeq proteins (2): NP_000944, NP_001268398 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR000376Pglndn_D_rcptFamily
IPR008365Prostanoid_rcptFamily
IPR017452GPCR_Rhodpsn_7TMDomain

Pfam: PF00001

UniProt features (26 total): topological domain 8, transmembrane region 7, sequence variant 4, glycosylation site 3, splice variant 2, chain 1, disulfide bond 1

Structure

Experimental structures (PDB)

8 structures.

PDBMethodResolution (Å)
8ZVZELECTRON MICROSCOPY2.35
9AU0ELECTRON MICROSCOPY2.45
9E9SELECTRON MICROSCOPY2.68
8ZW0ELECTRON MICROSCOPY2.72
9EI5ELECTRON MICROSCOPY2.84
9EE5ELECTRON MICROSCOPY2.89
9EKHELECTRON MICROSCOPY2.89
9UWDELECTRON MICROSCOPY3.41

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q13258-F179.060.39

Antibody-complex structures (SAbDab): 3 — 8ZW0, 9E9S, 9EI5

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): 105–183

Glycosylation sites (3): 10, 90, 297

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-391908Prostanoid ligand receptors
R-HSA-418555G alpha (s) signalling events

MSigDB gene sets: 193 (showing top): GSE45365_HEALTHY_VS_MCMV_INFECTION_CD8_TCELL_IFNAR_KO_DN, BENPORATH_ES_WITH_H3K27ME3, GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_CELLULAR_RESPONSE_TO_PROSTAGLANDIN_STIMULUS, GOBP_MALE_SEX_DETERMINATION, GOBP_SEX_DETERMINATION, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_LEUKOCYTE_MEDIATED_IMMUNITY, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_CELL_ACTIVATION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_MAST_CELL_ACTIVATION

GO Biological Process (9): inflammatory response (GO:0006954), G protein-coupled receptor signaling pathway (GO:0007186), positive regulation of cytosolic calcium ion concentration (GO:0007204), male sex determination (GO:0030238), sleep (GO:0030431), mast cell degranulation (GO:0043303), adenosine metabolic process (GO:0046085), cellular response to prostaglandin D stimulus (GO:0071799), signal transduction (GO:0007165)

GO Molecular Function (4): prostaglandin J receptor activity (GO:0001785), prostaglandin D receptor activity (GO:0004956), 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:

CategoryPathways
Eicosanoid ligand-binding receptors1
GPCR downstream signalling1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
prostaglandin receptor activity2
defense response1
G protein-coupled receptor activity1
signal transduction1
regulation of biological quality1
multicellular organism development1
sex determination1
multicellular organismal process1
mast cell activation involved in immune response1
mast cell mediated immunity1
lysosome localization1
leukocyte degranulation1
establishment of organelle localization1
purine ribonucleoside metabolic process1
cellular response to prostaglandin stimulus1
response to prostaglandin D1
cellular response to alcohol1
cellular response to ketone1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
transmembrane signaling receptor activity1
G protein-coupled receptor signaling pathway1
binding1
membrane1
cell periphery1
cellular anatomical structure1

Protein interactions and networks

STRING

1416 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PTGDRPTGDR2Q9Y5Y4852
PTGDRPTGDSP41222841
PTGDREZH2Q15910817
PTGDRPDS5BQ9NTI5816
PTGDRWDR5P61964708
PTGDRHPGDSO60760692
PTGDRAGO2Q9UKV8611
PTGDRDCST1Q5T197600
PTGDRZEB1P37275576
PTGDRAFAP1Q8N556570
PTGDRNPSR1Q6W5P4556
PTGDRMETTL3Q86U44548
PTGDRCCKP06307544
PTGDRRUNX2Q13950534
PTGDRRHPN1Q8TCX5528

IntAct

20 interactions, top by confidence:

ABTypeScore
GGA3PTGDRpsi-mi:“MI:0915”(physical association)0.610
PTGDRGGA3psi-mi:“MI:0915”(physical association)0.610
GGA3PTGDRpsi-mi:“MI:0403”(colocalization)0.610
SCRIBPTGDRpsi-mi:“MI:0407”(direct interaction)0.440
SNTA1PTGDRpsi-mi:“MI:0407”(direct interaction)0.440
PTGDRPTGDSpsi-mi:“MI:0915”(physical association)0.400
PTGDRRAMP1psi-mi:“MI:0915”(physical association)0.400
RAMP2PTGDRpsi-mi:“MI:0915”(physical association)0.400
RAMP3PTGDRpsi-mi:“MI:0915”(physical association)0.400
RAMP1PTGDRpsi-mi:“MI:0915”(physical association)0.400
PTGDRRAMP3psi-mi:“MI:0915”(physical association)0.400
PTGDRRAMP2psi-mi:“MI:0915”(physical association)0.400
PTGDRP4HBpsi-mi:“MI:0403”(colocalization)0.270

BioGRID (20): PTGDS (Affinity Capture-Western), HSP90AA1 (Affinity Capture-Western), MAPK1 (Affinity Capture-Western), MAPK3 (Affinity Capture-Western), PTGDR2 (Affinity Capture-Western), PTGDR (Affinity Capture-Western), SMARCA4 (Affinity Capture-Western), E2F6 (Affinity Capture-Western), GGA3 (Affinity Capture-Western), PTGDR (Affinity Capture-Western), GGA3 (Reconstituted Complex), PTGDR (Reconstituted Complex), APP (Reconstituted Complex), ANKRD13C (Reconstituted Complex), ANKRD13C (Affinity Capture-Western)

ESM2 similar proteins: A5D7K8, O35932, O95136, O95977, P21731, P30557, P30987, P34972, P34978, P34979, P34980, P35375, P35408, P37289, P43088, P43114, P43115, P43116, P43117, P43118, P43119, P43252, P43253, P46069, P47752, P47901, P47936, P50131, P52592, P56486, P70263, P70597, P79393, Q13258, Q28691, Q28905, Q5R949, Q62053, Q62928, Q8MJ08

Diamond homologs: A5D7K8, O35932, P34978, P43116, P43119, P43252, P43253, P70263, P79393, Q13258, Q62053, Q62928, Q9R261, Q9XT82, P32240, P35408, P43114, Q28691, Q8MJ08, Q95KZ0, D4A7K7, O08556, O18793, O55193, O62743, O97571, O97878, O97879, O97880, O97881, O97882, O97883, O97962, O97975, P21109, P30557, P32249, P33396, P34975, P34979

SIGNOR signaling

3 interactions.

AEffectBMechanism
PTGDR“up-regulates activity”GNASbinding
PTGDR“up-regulates activity”GNALbinding
“prostaglandin D2(1-)”“up-regulates activity”PTGDR“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance55
Likely benign6
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

247 predictions. Top by Δscore:

VariantEffectΔscore
14:52274729:A:AGacceptor_gain1.0000
14:52274730:G:GGacceptor_gain1.0000
14:52274730:GT:Gacceptor_gain1.0000
14:52274730:GTATC:Gacceptor_gain1.0000
14:52268661:G:GGdonor_gain0.9900
14:52274730:GTAT:Gacceptor_gain0.9800
14:52268568:G:Tdonor_gain0.9700
14:52274726:AACAG:Aacceptor_loss0.9700
14:52274727:ACAGT:Aacceptor_loss0.9700
14:52274728:CAG:Cacceptor_loss0.9700
14:52274729:A:Gacceptor_loss0.9700
14:52274730:GTA:Gacceptor_gain0.9700
14:52268658:ATT:Adonor_gain0.9600
14:52268659:TT:Tdonor_gain0.9600
14:52268688:GGCAC:Gdonor_gain0.9600
14:52274724:A:AGacceptor_gain0.9600
14:52268657:AATTG:Adonor_loss0.9500
14:52268659:T:Gdonor_gain0.9500
14:52268660:TGT:Tdonor_loss0.9500
14:52268661:GTGAG:Gdonor_loss0.9500
14:52268662:TG:Tdonor_loss0.9500
14:52268663:GAGTC:Gdonor_loss0.9500
14:52268664:AGT:Adonor_loss0.9500
14:52268665:G:Tdonor_loss0.9400
14:52269625:A:Tdonor_gain0.9400
14:52274126:A:Gdonor_gain0.9400
14:52274725:A:Gacceptor_gain0.9400
14:52268638:C:CGdonor_gain0.9300
14:52268781:A:Tdonor_gain0.9200
14:52274126:A:AGdonor_gain0.9100

AlphaMissense

2297 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
14:52274845:T:AW321R0.991
14:52274845:T:CW321R0.991
14:52268052:A:CS80R0.990
14:52268054:C:AS80R0.990
14:52268054:C:GS80R0.990
14:52268427:A:CS205R0.989
14:52268429:C:AS205R0.989
14:52268429:C:GS205R0.989
14:52268364:T:CF184L0.982
14:52268366:T:AF184L0.982
14:52268366:T:GF184L0.982
14:52267995:T:CF61L0.978
14:52267997:C:AF61L0.978
14:52267997:C:GF61L0.978
14:52268360:G:CW182C0.978
14:52268360:G:TW182C0.978
14:52274851:T:CF323L0.976
14:52274853:T:AF323L0.976
14:52274853:T:GF323L0.976
14:52268043:T:CC77R0.974
14:52267896:A:CS28R0.970
14:52267898:C:AS28R0.970
14:52267898:C:GS28R0.970
14:52268358:T:AW182R0.969
14:52268358:T:CW182R0.969
14:52268361:T:AC183S0.969
14:52268362:G:CC183S0.969
14:52268363:C:GC183W0.968
14:52274843:C:AP320H0.967
14:52268361:T:CC183R0.964

dbSNP variants (sampled 300 via entrez): RS1000376357 (14:52269413 G>A,T), RS1000661694 (14:52269634 A>C), RS1000798556 (14:52270085 C>T), RS1001289437 (14:52265814 T>C), RS1001329194 (14:52280412 C>T), RS1001592577 (14:52280164 C>T), RS1001961000 (14:52280672 T>C), RS1002044231 (14:52275115 A>T), RS1002121748 (14:52269079 C>T), RS1002549841 (14:52271797 A>G), RS1002791277 (14:52266696 C>A,T), RS1002820204 (14:52273037 T>A,C), RS1002848251 (14:52278858 C>G), RS1003024250 (14:52277551 C>G), RS1003068119 (14:52277831 T>G)

Disease associations

OMIM: gene MIM:604687 | disease phenotypes: MIM:607277

GenCC curated gene-disease

DiseaseClassificationInheritance
asthma-related traits, susceptibility to, 1LimitedAutosomal dominant

Mondo (1): asthma-related traits, susceptibility to, 1 (MONDO:0011805)

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 (1): CHEMBL4427 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

14 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 11,172 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1237119TREPROSTINIL4766
CHEMBL238804SELEXIPAG41,018
CHEMBL361812RAMATROBAN43,250
CHEMBL426559LAROPIPRANT4541
CHEMBL494ILOPROST4234
CHEMBL815DINOPROST43,118
CHEMBL2386081SETIPIPRANT3226
CHEMBL3301604RALINEPAG3260
CHEMBL3545043ASAPIPRANT3146
CHEMBL560993TIMAPIPRANT3285
CHEMBL1951575VIDUPIPRANT2890
CHEMBL239226LASELIPAG2314
CHEMBL551813BI-671800295
CHEMBL561132MK-7246129

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Prostanoid receptors

Most potent curated ligand interactions (32 total), top 25:

LigandActionAffinityParameter
laropiprantAntagonist10.1pKi
ZK110841Full agonist9.5pKi
[3H]PGD2Full agonist9.5pKd
BW 245CFull agonist9.4pKi
L-644,698Full agonist9.3pKi
BWA868CAntagonist9.3pKi
PGD2Full agonist9.2pKi
PGJ2Full agonist9.0pKi
S-5751Antagonist8.8pKi
[3H]BWA868CAntagonist8.8pKd
vidupiprantAntagonist8.4pIC50
treprostinilFull agonist8.4pKi
SQ-27986Full agonist8.0pKi
[3H]PGE2Agonist7.9pKd
ONO-AE3-237Antagonist7.7pKi
RS 93520Partial agonist7.5pKi
L-888,291Full agonist7.4pKi
ZK118182Full agonist7.3pKi
PGE1Full agonist7.3pKi
Δ12-PGJ2Full agonist7.0pKd
PGE2Full agonist7.0pKi
carbacyclinFull agonist6.9pKi
asapiprantAntagonist6.62pKi
15-deoxy-Δ12,14-PGJ2Full agonist6.6pKi
iloprostFull agonist6.6pKi

ChEMBL bioactivities

815 potent at pChembl≥5 of 842 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.70IC500.01995nMCHEMBL1644207
10.52Kd0.03nMLAROPIPRANT
10.30IC500.05012nMCHEMBL1644214
10.05IC500.09nMLAROPIPRANT
10.00IC500.1nMCHEMBL1644206
9.85IC500.14nMCHEMBL483991
9.66IC500.22nMCHEMBL484778
9.59IC500.26nMCHEMBL426387
9.57IC500.27nMCHEMBL116836
9.54IC500.29nMCHEMBL385126
9.52IC500.302nMCHEMBL1644213
9.52IC500.302nMCHEMBL1644245
9.51Ki0.31nMCHEMBL1290299
9.49Ki0.32nMCHEMBL483991
9.48Ki0.33nMCHEMBL1287835
9.48Ki0.33nMCHEMBL1290414
9.44Ki0.36nMCHEMBL1290298
9.44Ki0.36nMCHEMBL1290639
9.42Ki0.38nMCHEMBL1290080
9.42Ki0.38nMCHEMBL1290523
9.41Ki0.39nMCHEMBL484779
9.41Ki0.39nMCHEMBL520007
9.41Ki0.39nMCHEMBL1290755
9.40IC500.4nMCHEMBL116837
9.40IC500.3981nMCHEMBL1644211
9.40IC500.3981nMCHEMBL1644227
9.40IC500.3981nMCHEMBL1644247
9.39Ki0.41nMCHEMBL1290187
9.38IC500.42nMCHEMBL79943
9.37Ki0.43nMCHEMBL1290413
9.30IC500.5012nMCHEMBL1644208
9.30IC500.5012nMCHEMBL1644212
9.30IC500.5012nMCHEMBL1644253
9.29Ki0.51nMCHEMBL1290524
9.28Ki0.53nMCHEMBL483159
9.24Ki0.57nMLAROPIPRANT
9.24Ki0.57nMDIASTEREOMER 2
9.22EC500.6nMTREPROSTINIL
9.19Ki0.64nMCHEMBL484778
9.17Ki0.67nMCHEMBL484777
9.15Ki0.71nMCHEMBL483346
9.13Ki0.74nMCHEMBL483154
9.12Ki0.75nMCHEMBL1290079
9.10Ki0.8nMCHEMBL482744
9.10IC500.7943nMCHEMBL1644217
9.09IC500.81nMCHEMBL185251
9.06Ki0.88nMCHEMBL509685
9.06Ki0.88nMCHEMBL518988
9.05IC500.9nMCHEMBL311790
9.05Ki0.89nMCHEMBL1289984

PubChem BioAssay actives

676 with measured affinity, of 1133 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
2-[3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]phenyl]-2,2-difluoroacetic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic50<0.0001uM
2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid277844: Binding affinity to human DP receptor expressed in HEK293 cellskd<0.0001uM
4-[3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]phenyl]oxane-4-carboxylic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0001uM
2-[(6R)-5-(3,4-dichlorophenyl)sulfanyl-4-propan-2-yl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353262: Antagonist activity at DP1 in washed human platelet assessed as inhibition of PGD2-induced [125I]cAMP production preincubated 10 mins before PGD2 challenge by scintillation proximity assayic500.0001uM
N-[2-(2,4-dichlorophenyl)ethyl]-6-[3-[difluoro(2H-tetrazol-5-yl)methyl]phenyl]-2-methoxypyrimidin-4-amine552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0001uM
2-[(6S)-5-(3,4-dichlorophenyl)sulfanyl-4-propan-2-yl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353262: Antagonist activity at DP1 in washed human platelet assessed as inhibition of PGD2-induced [125I]cAMP production preincubated 10 mins before PGD2 challenge by scintillation proximity assayic500.0002uM
(Z)-7-[(1R,2R,3S,5S)-2-[(5-fluoro-1-benzothiophene-3-carbonyl)amino]-6,6-dimethyl-3-bicyclo[3.1.1]heptanyl]hept-5-enoic acid160532: Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesic500.0003uM
2-[(3R)-5-acetyl-4-[(4-chlorophenyl)methyl]-7-fluoro-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid277852: Activity at human DP receptor in washed platelets assessed as inhibition of PGD2-induced cAMP accumulationic500.0003uM
2-[(3R)-5-bromo-4-[(4-chlorophenyl)methyl]-7-fluoro-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid277852: Activity at human DP receptor in washed platelets assessed as inhibition of PGD2-induced cAMP accumulationic500.0003uM
2-[3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]phenyl]-2-methylpropanoic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0003uM
2-[(1R)-9-[(1S)-1-(3,4-dichlorophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0003uM
2-[(1R)-6-fluoro-9-[(1S)-1-(4-fluorophenyl)ethyl]-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0003uM
2-[(1R)-9-[(1S)-1-(3-chlorophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0003uM
3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]benzoic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0003uM
2-[5-(2,4-dichlorophenyl)sulfanyl-4-propan-2-yl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0004uM
2-[(1R)-9-[(1R)-1-(4-chlorophenyl)-2,2-difluoroethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-[(1R)-9-[(1R)-1-(4-chlorophenyl)-2-fluoroethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-[(1R)-6-fluoro-8-methylsulfonyl-9-[(1S)-1-[4-(trifluoromethyl)phenyl]ethyl]-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-fluoro-5-[2-methoxy-6-[2-(4-methoxyphenyl)ethylamino]pyrimidin-4-yl]benzoic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0004uM
2-[(1R)-9-[(1S)-1-(4-chloro-3-fluorophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
(E)-7-[(1R,2R,3S,5S)-2-[(5-fluoro-1-benzothiophene-3-carbonyl)amino]-6,6-dimethyl-3-bicyclo[3.1.1]heptanyl]hept-5-enoic acid160534: Prostaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranesic500.0004uM
2-[4-propan-2-yl-5-(2,4,5-trichlorophenyl)sulfanyl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0004uM
2-[(1R)-6-fluoro-8-methylsulfonyl-9-[(1S)-1-phenylethyl]-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-[(1R)-9-[(1S)-1-(4-chloro-2-fluorophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-[(1R)-9-[(1S)-1-(4-bromophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0004uM
2-methoxy-N-[2-(4-methoxyphenyl)ethyl]-6-[3-(2H-tetrazol-5-yl)phenyl]pyrimidin-4-amine552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0004uM
N-[2-(2,4-dichlorophenyl)ethyl]-2-methoxy-6-[3-[2-(2H-tetrazol-5-yl)propan-2-yl]phenyl]pyrimidin-4-amine552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0004uM
(Z)-7-[(1R,2R,3S,5S)-2-[(5-hydroxy-1-benzothiophene-3-carbonyl)amino]-6,6-dimethyl-3-bicyclo[3.1.1]heptanyl]hept-5-enoic acid160532: Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesic500.0004uM
2-[5-(3,4-dichlorophenyl)sulfanyl-4-propan-2-yl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0005uM
2-[(1R)-9-[(1S)-1-(4-cyanophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0005uM
2-[3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]-4-fluorophenyl]-2-methylpropanoic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0005uM
1-[3-[6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]phenyl]cyclopentane-1-carboxylic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0005uM
2-methoxy-N-[2-(4-methoxyphenyl)ethyl]-6-[4-methoxy-3-(2H-tetrazol-5-yl)phenyl]pyrimidin-4-amine552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0005uM
2-[4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid342293: Inhibition of prostaglandin DP receptorki0.0006uM
Treprostinil1872472: Agonist activity at human DP1 expressed in human 1321N1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisec500.0006uM
2-[5-(4-chlorophenyl)sulfanyl-4-propan-2-yl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0007uM
2-[4-(cyclopropylmethyl)-5-(3,4-dichlorophenyl)sulfanyl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0007uM
2-[4-propan-2-yl-5-[4-(trifluoromethyl)phenyl]sulfanyl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0007uM
2-[1-[4-[[(2S)-7-fluoro-4-methyl-2,3-dihydro-1,4-benzoxazin-2-yl]methoxy]benzoyl]-2-methylindol-4-yl]acetic acid248929: Effect on the increase in cAMP formation induced by PGD-2 in the presence of bovine serum albumin in CHO cells expressing human Prostaglandin D2 receptoric500.0008uM
2-[(1R)-9-[(1S)-1-(4-chlorophenyl)ethyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0008uM
3-[6-[2-(2,4-difluorophenyl)ethylamino]-2-methoxypyrimidin-4-yl]benzoic acid552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0008uM
2-[4-cyclopropyl-5-(3,4-dichlorophenyl)sulfanyl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0008uM
2-[9-[(4-chlorophenyl)methyl]-6-fluoro-8-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid540059: Antagonist activity at prostanoid DP1 receptorki0.0009uM
3-[2-methoxy-6-[2-(4-methoxyphenyl)ethylamino]pyrimidin-4-yl]benzonitrile552754: Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assayic500.0009uM
2-[5-(4-chlorophenyl)sulfanyl-4-propan-2-yl-6,7,8,9-tetrahydropyrido[3,2-b]indolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0009uM
2-[5-(3,4-dichlorophenyl)sulfanyl-4-ethyl-7,8-dihydro-6H-pyrido[4,3-e]pyrrolizin-6-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0009uM
2-[10-(3,4-dichlorophenyl)sulfanyl-1-propan-2-yl-6,7,8,9-tetrahydropyrido[3,4-b]indolizin-9-yl]acetic acid353253: Displacement of radioligand from human recombinant DP1 receptor expressed in HEK293 cells by scintillation proximity assayki0.0009uM
(E)-7-[(1R,2R,3S,5S)-2-[(5-hydroxy-1-benzothiophene-3-carbonyl)amino]-6,6-dimethyl-3-bicyclo[3.1.1]heptanyl]hept-5-enoic acid222781: Concentration required to inhibit the PGD-2 evoked cAMP formation in human plateletsic500.0009uM
2-[9-[(4-chlorophenyl)methyl]-8-methylsulfanyl-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid266351: Binding affinity to DP receptorki0.0010uM
2-[5-bromo-4-[(7-chloroquinolin-2-yl)methyl]-7-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid266351: Binding affinity to DP receptorki0.0010uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
MK-0524affects binding, decreases activity, decreases response to substance13
Prostaglandin D2affects binding, decreases reaction, increases activity2
Dinoprostoneaffects binding, increases activity, decreases reaction2
Dinoprostaffects binding, increases activity, decreases reaction2
GSK-J4decreases expression1
methylmercuric chloridedecreases expression1
triphenyl phosphateaffects expression1
trichostatin Adecreases expression1
butyraldehydedecreases expression1
adenosine 5’-O-(3-thiotriphosphate)affects binding, decreases reaction1
BW 245Caffects binding, increases activity, decreases reaction1
13,14-dihydro-15-ketoprostaglandin D2affects binding, increases activity, decreases reaction1
9-deoxy-delta-9-prostaglandin D2decreases reaction, affects binding, increases activity1
pentanaldecreases expression1
BW A868Caffects binding, increases activity, decreases reaction1
ZK 110841affects binding, increases activity, decreases reaction1
di-n-butylphosphoric acidaffects expression1
CGP 52608affects binding, increases reaction1
15-deoxy-delta(12,14)-prostaglandin J2affects binding, increases activity, decreases reaction1
L 644698affects binding, increases activity, decreases reaction1
delta(12)-prostaglandin J(2)affects binding, increases activity, decreases reaction1
MT19c compounddecreases expression1
Resveratrolaffects cotreatment, decreases expression1
Adenylyl Imidodiphosphateaffects binding, decreases reaction1
Alprostadilaffects binding, decreases reaction1
Benzo(a)pyreneincreases methylation1
Copperaffects cotreatment, decreases expression1
Diethylhexyl Phthalatedecreases expression1
Guanylyl Imidodiphosphateaffects binding, decreases reaction1
Niacinaffects binding, decreases activity, decreases response to substance1

ChEMBL screening assays

131 unique, capped per target: 91 binding, 40 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1047088BindingDisplacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation countingDiscovery and optimization of CRTH2 and DP dual antagonists. — Bioorg Med Chem Lett
CHEMBL1047103FunctionalAntagonist activity at DP receptor in human platelets assessed as inhibition of PGD2-induced cAMP production by competitive ELISADiscovery and optimization of CRTH2 and DP dual antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

3 cell lines: 3 spontaneously immortalized cell line

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

CellosaurusNameCategorySex
CVCL_H424CHO-K1/DP1/Galpha15Spontaneously immortalized cell lineFemale
CVCL_KV67cAMP Hunter CHO-K1 PTGDR GsSpontaneously immortalized cell lineFemale
CVCL_ZI80GeneBLAzer PTGDR-CRE-bla CHO-K1Spontaneously immortalized cell lineFemale

Clinical trials (associated diseases)

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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 80

This page pulls from 80 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot