PTGER2

Summary

PTGER2 (prostaglandin E receptor 2, HGNC:9594) is a protein-coding gene on chromosome 14q22.1, encoding Prostaglandin E2 receptor EP2 subtype (P43116). Receptor for prostaglandin E2 (PGE2).

This gene encodes a receptor for prostaglandin E2, a metabolite of arachidonic acid which has different biologic activities in a wide range of tissues. Mutations in this gene are associated with aspirin-induced susceptibility to asthma.

Source: NCBI Gene 5732 — RefSeq curated summary.

At a glance

• Gene–disease (curated): asthma, nasal polyps, and aspirin intolerance (Limited, GenCC)
• Clinical variants (ClinVar): 44 total
• Phenotypes (HPO): 5
• Druggable target: yes — 16 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000956

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9594
Approved symbol	PTGER2
Name	prostaglandin E receptor 2
Location	14q22.1
Locus type	gene with protein product
Status	Approved
Aliases	EP2, COX-2
Ensembl gene	ENSG00000125384
Ensembl biotype	protein_coding
OMIM	176804
Entrez	5732

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000245457, ENST00000557436

RefSeq mRNA: 1 — MANE Select: NM_000956 NM_000956

CCDS: CCDS9708

Canonical transcript exons

ENST00000245457 — 2 exons

Exon	Start	End
ENSE00000854727	52314312	52315391
ENSE00000854728	52327221	52328598

Expression profiles

Bgee: expression breadth ubiquitous, 178 present calls, max score 96.09.

FANTOM5 (CAGE): breadth broad, TPM avg 11.8312 / max 899.3004, expressed in 913 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139606	10.4769	888
139605	0.9571	282
139608	0.1536	81
139607	0.1461	65
139609	0.0976	59

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	96.09	gold quality
leukocyte	CL:0000738	92.57	gold quality
monocyte	CL:0000576	92.46	gold quality
mononuclear cell	CL:0000842	92.38	gold quality
cartilage tissue	UBERON:0002418	90.90	gold quality
blood	UBERON:0000178	88.33	gold quality
bone marrow	UBERON:0002371	85.94	gold quality
bone marrow cell	CL:0002092	83.43	gold quality
endocervix	UBERON:0000458	82.51	gold quality
mucosa of stomach	UBERON:0001199	82.11	gold quality
trabecular bone tissue	UBERON:0002483	81.90	silver quality
vermiform appendix	UBERON:0001154	79.83	gold quality
spleen	UBERON:0002106	79.60	gold quality
calcaneal tendon	UBERON:0003701	79.32	gold quality
stromal cell of endometrium	CL:0002255	78.87	gold quality
body of stomach	UBERON:0001161	78.51	gold quality
caecum	UBERON:0001153	77.85	gold quality
body of uterus	UBERON:0009853	77.85	gold quality
gall bladder	UBERON:0002110	77.72	gold quality
stomach	UBERON:0000945	77.23	gold quality
rectum	UBERON:0001052	77.22	gold quality
pigmented layer of retina	UBERON:0001782	77.14	gold quality
mucosa of paranasal sinus	UBERON:0005030	76.98	silver quality
bronchial epithelial cell	CL:0002328	76.94	gold quality
omental fat pad	UBERON:0010414	76.83	gold quality
peritoneum	UBERON:0002358	76.78	gold quality
mucosa of sigmoid colon	UBERON:0004993	76.45	gold quality
adipose tissue of abdominal region	UBERON:0007808	76.42	gold quality
germinal epithelium of ovary	UBERON:0001304	76.26	silver quality
myometrium	UBERON:0001296	75.81	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-HCAD-11	yes	41.87
E-CURD-122	yes	27.51
E-ANND-3	yes	7.84
E-MTAB-7606	no	1397.09
E-GEOD-124858	no	49.75
E-HCAD-30	no	43.81

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AR, CREM, MNX1, MYC, PGR, PPARG, RORC, SETBP1

miRNA regulators (miRDB)

71 targeting PTGER2, 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-3163	100.00	77.23	8605
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-511-3P	99.99	68.85	1467
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-3671	99.90	73.04	3897
HSA-MIR-30A-3P	99.87	69.74	2928
HSA-MIR-30D-3P	99.87	69.92	2917
HSA-MIR-30E-3P	99.87	69.68	2942
HSA-MIR-3941	99.86	70.54	2735
HSA-MIR-548AR-3P	99.85	71.26	3889
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-4420	99.82	70.08	1624
HSA-MIR-548AZ-3P	99.82	70.56	3549
HSA-MIR-548BC	99.82	70.61	3524
HSA-MIR-548E-3P	99.82	70.59	3514
HSA-MIR-548F-3P	99.82	70.59	3540
HSA-MIR-181B-2-3P	99.81	70.06	1646

Literature-anchored findings (GeneRIF, showing 40)

• PGE(2) receptors and synthesis in human gastric mucosa: perturbation in cancer (PMID:12051958)
• effects of PGE2 on monocyte-derived dendritic cells were mediated through increased cyclic adenosine monophosphate by 2 of the known PGE2 receptors, EP2 and EP4 (PMID:12149218)
• Activation of prostaglandin E2-receptor EP2 and EP4 pathways induces growth inhibition in human gastric carcinoma cell lines. (PMID:12228765)
• Data show that down-regulation of prostaglandin E(2) receptor subtype EP(2) receptors represents a potential mechanism for neoplastic progression to an invasive phenotype. (PMID:12466123)
• shear activates cyclooxygenase-2, via a c-Jun N-terminal kinase2/c-Jun-dependent pathway, which in turn elicits downstream prostaglandin EP2 and EP3a1 receptor mRNA synthesis (PMID:12743126)
• Agonists of EP(1) and EP(2) significantly increased aromatase activity levels, which were decreased by the corresponding antagonists. Generally reflective of changes in aromatase protein expression and the pattern of mRNA expression. (PMID:12788892)
• increased histone H3 acetylation involving the EP2 receptor, protein kinase A, CREB, and CREB binding protein is responsible for PGE(2)-induced StAR gene activation in endometriotic stromal cells. (PMID:12933667)
• COX-2 induction by bradykinin in human pulmonary artery smooth muscle cells is mediated by the cyclic AMP response element through a novel autocrine loop involving endogenous prostaglandin E2, EP2 receptor, and EP4 receptor (PMID:14517215)
• Human corpus cavernosum and cultured smooth muscle cells express EP1, EP2 and EP3 receptors. (PMID:14562138)
• role of araomatic amino acids in i2 loop in Gs coupling (PMID:14699136)
• elevated EP2 receptor expression may facilitate the PGE(2)-induced release of proangiogenic factors in reproductive tumor cells via intracellular cAMP-mediated transactivation of the EGFR and ERK1/2 pathways (PMID:15044590)
• Endothelin-1-induced prostaglandin E2-EP2 and EP4 signaling regulates vascular endothelial growth factor production and ovarian carcinoma cell invasion (PMID:15347673)
• PGE2, via EP2 receptor, enhances PTEN function in lung fibroblasts to inhibit directional migration (PMID:15539459)
• PGE2 increases VEGF transcriptionally and involves the Sp-1 binding site via a cAMP-dependent mechanism involving EP2 and EP4 receptors (PMID:15970595)
• a novel proinflammatory and proamyloidogenic function for the PGE2 EP2 receptor is demonstrated in a model of familial Alzheimer’s disease. (PMID:16267225)
• significantly reduced expression of PGE(2) receptors on nasal mucosa inflammatory leukocytes in the aspirin-sensitive compared with nonaspirin-sensitive rhinosinusitis patients (PMID:16461132)
• Together, the results suggest that the overexpression of the human EP2 receptor plays a significant role in the protumorigenic action of PGE2 in mouse skin. (PMID:16607275)
• prostaglandin-endoperoxide synthase 2 polymorphisms, prostaglandin-E receptor 2 polymorphisms, and C-reactive protein concentrations may have a role in atherothrombosis (PMID:16879213)
• These data indicate that PGE(2) inhibits fibroblast activation in primary lung fibroblasts via binding of EP2 receptor and production of cyclic AMP; inhibition of collagen I proceeds via activation of PKA. (PMID:17028262)
• These results suggest that the COX-2-PGE(2) pathway may be involved in IL-8 production in gastric epithelial cells. (PMID:17078003)
• EP2 mRNA was significantly higher in normal colon tissue compared with tumor tissue. (PMID:17290397)
• Selective stimulation of the EP2 receptor subtype, leading to epidermal growth factor receptor (EGFR) transactivation via protein kinase A (PMID:17384145)
• participates in placentation through EVT invasion by up-regulating PGE2 production and PGE2 receptor expression in first trimester extravillous trophoblasts (PMID:17525067)
• NB cells may lose responsiveness to PTGER2-mediated growth inhibition/apoptosis through epigenetic silencing of PTGER2 and/or disruption of downstream cAMP-dependent pathway during the neuroblastomagenesis. (PMID:17533365)
• treatment of LS174T cells with indomethacin causes a down regulation of EP2 prostanoid receptors (PMID:17555711)
• Results show co-expression of cyclooxygenase-2 and prostaglandin E2 receptors EP1, 2 and 4 in non-small cell lung cancer cells concomitant with the synthesis of PGE2. (PMID:17611676)
• Role of EP2 receptor in mediating the PGE2 effect on stimulating cyst formation may have direct pharmacological implications for the treatment of polycystic kidney disease. (PMID:17728378)
• 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)
• herpes simplex virus type 1 infected mature monocyte-derived dendritic cells demonstrated a dramatic down-regulation of the expression of the EP2 and EP4 receptors (PMID:18086382)
• PGE2 receptors were expressed in both NCI-H292 and human nasal epithelial cells. (PMID:18254372)
• results showed that EP2 is expressed in trigeminal neurons (58% of total neurons) and is co-expressed in TRPV(1)-positive neurons (64% of TRPV(1)-positive neurons. (PMID:18296611)
• CCR7 and the EP2/EP4 receptor signaling pathway are down-stream targets for COX-2 to enhance the migration of breast cancer cells toward LECs and to promote lymphatic invasion (PMID:18319253)
• Prostaglandin E(2), via the prostanoid receptor EP2 and subsequent cAMP elevation, downregulates mRNA and protein levels of protease-activated receptor-1 in human lung fibroblasts. (PMID:18537828)
• PTGER2 methylation was present with greater frequency in nonsmall cell lung cancer with EGFR mutation. (PMID:18666211)
• A new approach for blocking E-prostanoid receptor-mediated cell signaling using a soluble chimeric EP2 fragment, is described. (PMID:18790761)
• findings show the G(s)-coupled EP(2) receptor closes K(Ca)3.1 in lung mast cells and attenuates both chemokine- and PGE(2)-dependent lung mast cell migration (PMID:18792407)
• PGE(2) induces angiogenesis in prostate cancer through EP2 and EP4. (PMID:18829529)
• Common polymorphisms of cyclooxygenase-2 and prostaglandin E2 receptor and increased risk for acute coronary syndrome in coronary artery disease. (PMID:18989535)
• Overexpression of EP2 is associated with esophageal squamous cell carcinoma. (PMID:19050969)
• Results suggest that prostaglandin E2 mainly induces the activation of beta(1)-integrins via the EP(2) receptor in human coronary arterial endothelial cells. (PMID:19169646)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ptger2a	ENSDARG00000011434
danio_rerio	ptger2b	ENSDARG00000037033
mus_musculus	Ptger2	ENSMUSG00000037759
rattus_norvegicus	Ptger2	ENSRNOG00000050968

Paralogs (7): TBXA2R (ENSG00000006638), PTGER3 (ENSG00000050628), PTGFR (ENSG00000122420), PTGIR (ENSG00000160013), PTGER1 (ENSG00000160951), PTGDR (ENSG00000168229), PTGER4 (ENSG00000171522)

Protein

Protein identifiers

Prostaglandin E2 receptor EP2 subtype — P43116 (reviewed: P43116)

Alternative names: Prostanoid EP2 receptor

All UniProt accessions (2): P43116, G3V2Y6

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. The subsequent raise in intracellular cAMP is responsible for the relaxing effect of this receptor on smooth muscle.

Subcellular location. Cell membrane.

Tissue specificity. Placenta and lung.

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

RefSeq proteins (1): NP_000947* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR001923	Prostglndn_EP2_rcpt	Family
IPR008365	Prostanoid_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (43 total): helix 13, topological domain 8, transmembrane region 7, glycosylation site 4, strand 4, turn 3, chain 1, region of interest 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
7CX2	ELECTRON MICROSCOPY	2.8
7CX3	ELECTRON MICROSCOPY	2.8
7CX4	ELECTRON MICROSCOPY	2.9
9JRT	ELECTRON MICROSCOPY	3.28
9JRO	ELECTRON MICROSCOPY	3.5

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P43116-F1	78.06	0.35

Antibody-complex structures (SAbDab): 3 — 7CX2, 7CX3, 7CX4

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): 109–187

Glycosylation sites (4): 3, 6, 96, 287

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

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

MSigDB gene sets: 375 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, BENPORATH_ES_WITH_H3K27ME3, GOBP_RESPONSE_TO_PROSTAGLANDIN_E, GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_CELLULAR_RESPONSE_TO_PROSTAGLANDIN_STIMULUS, BROWNE_HCMV_INFECTION_16HR_UP, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, ZHAN_MULTIPLE_MYELOMA_CD1_UP, CTAGGAA_MIR384, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, MODULE_289, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_RESPONSE_TO_PROSTAGLANDIN

GO Biological Process (10): inflammatory response (GO:0006954), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), positive regulation of cytosolic calcium ion concentration (GO:0007204), response to nematode (GO:0009624), response to lipopolysaccharide (GO:0032496), response to progesterone (GO:0032570), regulation of cell population proliferation (GO:0042127), cellular response to prostaglandin E stimulus (GO:0071380), signal transduction (GO:0007165)

GO Molecular Function (2): prostaglandin E receptor activity (GO:0004957), 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
Eicosanoid ligand-binding receptors	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of cellular process	2
defense response	1
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
regulation of biological quality	1
response to other organism	1
response to molecule of bacterial origin	1
response to lipid	1
response to oxygen-containing compound	1
response to steroid hormone	1
response to ketone	1
cell population proliferation	1
response to prostaglandin E	1
cellular response to prostaglandin stimulus	1
cellular response to alcohol	1
cellular response to ketone	1
cell communication	1
cellular process	1
signaling	1
cellular response to stimulus	1
prostaglandin 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

936 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PTGER2	PTGES	O14684	736
PTGER2	PTGS2	P35354	695
PTGER2	PTGS1	P23219	610
PTGER2	CYS1	Q717R9	599
PTGER2	PTGER4	P35408	594
PTGER2	CXCL14	O95715	588
PTGER2	LTC4S	Q16873	576
PTGER2	AKR1C3	P42330	563
PTGER2	PTGER3	P43115	537
PTGER2	SLCO2A1	Q92959	537
PTGER2	PKHD1	P08F94	520
PTGER2	PTGFR	P43088	507
PTGER2	PTGES2	Q9H7Z7	485
PTGER2	TLR2	O60603	460
PTGER2	PTGER1	P34995	442

IntAct

4 interactions, top by confidence:

A	B	Type	Score
APP	PTGER2	psi-mi:“MI:0915”(physical association)	0.400
PTGER2	ARRB2	psi-mi:“MI:0914”(association)	0.350
PTGER2	cpdB	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (2): PTGER2 (Affinity Capture-Western), PTGER2 (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, P21731, P30557, P30987, P34979, P34980, P34995, P35375, P37289, P43088, P43115, P43117, P43118, P46069, P50131, P56486, P70597, Q1JPS6, Q28550, Q28905, Q5YKK9

SIGNOR signaling

6 interactions.

A	Effect	B	Mechanism
“prostaglandin E2”	up-regulates	PTGER2	“chemical activation”
PTGER2	up-regulates	GNAS	binding
PTGER2	up-regulates	EGFR
PTGER2	“up-regulates activity”	GNAS	binding
PTGER2	“up-regulates activity”	GNAL	binding
“prostaglandin E2(1-)”	“up-regulates activity”	PTGER2	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	38
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

272 predictions. Top by Δscore:

Variant	Effect	Δscore
14:52315388:CACGG:C	donor_loss	1.0000
14:52315389:ACGGT:A	donor_loss	1.0000
14:52315390:CGGT:C	donor_loss	1.0000
14:52315391:GGTA:G	donor_loss	1.0000
14:52315390:CG:C	donor_gain	0.9900
14:52315391:GG:G	donor_gain	0.9900
14:52315392:G:GC	donor_loss	0.9900
14:52315392:G:GG	donor_gain	0.9900
14:52315393:T:G	donor_loss	0.9900
14:52318663:T:TA	donor_gain	0.9900
14:52318664:A:AA	donor_gain	0.9900
14:52315387:TCACG:T	donor_gain	0.9800
14:52325765:T:G	acceptor_gain	0.9800
14:52327215:TTACA:T	acceptor_loss	0.9800
14:52327216:TACAG:T	acceptor_loss	0.9800
14:52327217:ACAG:A	acceptor_loss	0.9800
14:52327218:CA:C	acceptor_loss	0.9800
14:52327219:A:AG	acceptor_gain	0.9800
14:52327219:AG:A	acceptor_loss	0.9800
14:52327220:G:GG	acceptor_gain	0.9800
14:52315388:CACG:C	donor_gain	0.9700
14:52315389:ACG:A	donor_gain	0.9700
14:52321161:A:T	donor_gain	0.9600
14:52325764:A:AG	acceptor_gain	0.9600
14:52321160:GAAAA:G	donor_gain	0.9400
14:52324243:G:GT	donor_gain	0.9100
14:52318661:A:AG	donor_gain	0.9000
14:52318662:G:GG	donor_gain	0.9000
14:52321208:C:T	donor_gain	0.8400
14:52325764:AT:A	acceptor_gain	0.8400

AlphaMissense

2286 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:52314804:A:C	S86R	0.999
14:52314806:C:A	S86R	0.999
14:52314806:C:G	S86R	0.999
14:52327314:T:A	W313R	0.998
14:52327314:T:C	W313R	0.998
14:52314642:T:C	F32L	0.997
14:52314644:C:A	F32L	0.997
14:52314644:C:G	F32L	0.997
14:52327303:T:A	I309K	0.997
14:52314630:A:C	S28R	0.996
14:52314632:C:A	S28R	0.996
14:52314632:C:G	S28R	0.996
14:52314781:A:C	D78A	0.996
14:52314782:C:A	D78E	0.996
14:52314782:C:G	D78E	0.996
14:52314795:T:C	C83R	0.996
14:52314906:A:C	S120R	0.996
14:52314908:C:A	S120R	0.996
14:52314908:C:G	S120R	0.996
14:52315106:G:C	W186C	0.996
14:52315106:G:T	W186C	0.996
14:52315110:T:C	F188L	0.996
14:52315112:C:A	F188L	0.996
14:52315112:C:G	F188L	0.996
14:52315107:T:A	C187S	0.995
14:52315107:T:C	C187R	0.995
14:52315108:G:C	C187S	0.995
14:52315109:C:G	C187W	0.995
14:52327303:T:G	I309R	0.995
14:52327312:C:A	P312H	0.995

dbSNP variants (sampled 300 via entrez): RS1000084931 (14:52314287 G>A,C), RS1000481160 (14:52322574 T>C), RS1000698474 (14:52324159 A>C), RS1000703813 (14:52323910 T>C), RS1000918468 (14:52317647 G>A,C,T), RS1001216875 (14:52322006 C>A), RS1001263158 (14:52324275 G>C), RS1001371782 (14:52321268 T>TC), RS1001412916 (14:52321470 TTTTGAAGAGAAATC>T), RS1001883643 (14:52327693 A>T), RS1001969365 (14:52322955 T>C), RS1002065896 (14:52316883 G>A), RS1002117155 (14:52316387 A>T), RS1002216076 (14:52323255 A>G,T), RS1002500475 (14:52317177 A>G,T)

Disease associations

OMIM: gene MIM:176804 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
asthma, nasal polyps, and aspirin intolerance	Limited	Autosomal dominant

Mondo (2): asthma, aspirin-induced, susceptibility to (MONDO:0800415), asthma, nasal polyps, and aspirin intolerance (MONDO:0008834)

Orphanet (0):

HPO phenotypes

5 total (5 of 5 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0002099	Asthma
HP:0012042	Aspirin-induced asthma
HP:0100582	Nasal polyposis
HP:4000007	Bronchoconstriction

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1881 (SINGLE PROTEIN), CHEMBL2363068 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

16 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 19,016 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1237119	TREPROSTINIL	4	766
CHEMBL426559	LAROPIPRANT	4	541
CHEMBL4297666	OMIDENEPAG ISOPROPYL	4	107
CHEMBL494	ILOPROST	4	234
CHEMBL548	DINOPROSTONE	4	14,939
CHEMBL2386081	SETIPIPRANT	3	226
CHEMBL3301604	RALINEPAG	3	260
CHEMBL114395	PINADOLINE	2	462
CHEMBL2105692	TAPRENEPAG ISOPROPYL	2	19
CHEMBL2107783	TAPRENEPAG	2	29
CHEMBL2220404	CLOPROSTENOL	2
CHEMBL271896	BUTAPROST	2	1,116
CHEMBL3670685	PALUPIPRANT	2	53
CHEMBL3707245	OMIDENEPAG	2	81
CHEMBL563646	EVATANEPAG	2	145
CHEMBL3286797	PF-04418948	1	38

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1353411	Toxicity	3	aspirin	Asthma
rs2075797	Toxicity	3	aspirin	Asthma

PharmGKB variants

2 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1353411	PTGER2	3	1.50	1	aspirin
rs2075797	PTGER2	3	1.00	1	aspirin

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Prostanoid receptors

Most potent curated ligand interactions (37 total), top 25:

Ligand	Action	Affinity	Parameter
TG4-155	Antagonist	8.62	pKB
TG7-171	Antagonist	8.57	pKB
PF-04852946	Antagonist	8.53	pKB
ONO-AE1-259	Full agonist	8.5	pKi
omidenepag	Agonist	8.44	pKi
treprostinil	Full agonist	8.4	pKi
PGN-9856	Agonist	8.3	pKi
PGE2	Full agonist	8.3	pKi
PF-04418948	Antagonist	8.3	pKB
TG6-129	Antagonist	8.06	pKB
PGE1	Full agonist	8.04	pKi
TG11-77	Antagonist	8.01	pKB
taprenepag	Full agonist	8.0	pIC50
TG8-260	Antagonist	7.9	pKB
[3H]PGE2	Full agonist	7.9	pKd
16,16-dimethyl-PGE2	Full agonist	7.8	pKi
misoprostol (free acid form)	Full agonist	7.5	pKi
evatanepag	Full agonist	7.3	pIC50
11-deoxy-PGE1	Full agonist	7.3	pKi
butaprost (free acid form)	Full agonist	7.0	pKi
rivenprost	Full agonist	6.2	pKi
17-phenyl-ω-trinor-PGE2	Full agonist	6.1	pKi
PGF2α	Full agonist	6.0	pKi
carbacyclin	Full agonist	6.0	pKi
MB-28767	Full agonist	6.0	pKi

Binding affinities (BindingDB)

154 measured of 212 human assays (213 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[2-[1-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2,3-dihydroindol-7-yl]ethyl]benzoic acid	KI	0.3 nM	US-9546162: Compounds and methods for skin repair
NSC_5311503	KI	0.3 nM
NSC_3080928	KI	0.4 nM
2-[[6-[[[4-[3-[(E)-prop-1-enyl]phenyl]phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.53 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-ethoxyphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.61 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-prop-1-ynylphenyl)phenyl]methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.75 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(2-prop-1-ynylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.75 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-ethoxyphenyl)phenyl]methyl-thiophen-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.79 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-prop-1-ynylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.8 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-ethoxyphenyl)phenyl]methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.8 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-prop-1-ynylphenyl)phenyl]methyl-thiophen-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.9 nM	US-9676720: Substituted biaryl compound
2-[3-[[5-(3-fluorophenyl)-2-methoxy-3-methylphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	0.9 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[[6-[[[4-(6-ethoxy-2-pyridinyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.94 nM	US-9676720: Substituted biaryl compound
2-[[6-[[benzenesulfonyl-[[4-(3-prop-1-ynylphenyl)phenyl]methyl]amino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.95 nM	US-9676720: Substituted biaryl compound
2-[[6-[[benzenesulfonyl-[[4-(3-ethoxyphenyl)phenyl]methyl]amino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.97 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-prop-1-ynylphenyl)phenyl]methyl-thiophen-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	0.99 nM	US-9676720: Substituted biaryl compound
2-[3-[[3-(3-fluorophenyl)-5-hydroxyphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	1 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[[6-[[[4-(3-propylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.1 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-methoxyphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.2 nM	US-9676720: Substituted biaryl compound
2-[[6-[[(3-fluorophenyl)sulfonyl-[[4-(3-prop-1-ynylphenyl)phenyl]methyl]amino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.4 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-ethylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.4 nM	US-9676720: Substituted biaryl compound
3-(4-fluorophenyl)-N-[[5-(hydroxycarbamoyl)furan-2-yl]methyl]-5-phenyl-1H-pyrrole-2-carboxamide	KI	1.5 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[[6-[[(4-phenylphenyl)methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.5 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-[3-[(E)-but-1-enyl]phenyl]phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.5 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(3-prop-2-enylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	1.7 nM	US-9676720: Substituted biaryl compound
CAS_41598-07-6	KI	1.7 nM
3-(4-fluorophenyl)-5-thiophen-2-yl-1H-pyrrole-2-carboxylic acid	KI	1.9 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[[6-[[[4-(6-propoxy-2-pyridinyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	2 nM	US-9676720: Substituted biaryl compound
2-[2,4-difluoro-3-[[5-(3-fluorophenyl)-2,3-dimethylphenyl]methylamino]phenoxy]acetic acid	EC50	2 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[4-fluoro-3-[[2-fluoro-5-(3-fluorophenyl)-3-methylphenyl]methylamino]-2-methylphenoxy]acetic acid	EC50	2 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[3-[[5-(3-fluorophenyl)-2,3-dimethylphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	2 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[3-[[5-(3,4-difluorophenyl)-2,3-dimethylphenyl]methylamino]-2,4-difluorophenoxy]acetic acid	EC50	2 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
4-[2-[1-[(3-fluorophenyl)methyl]-2,3-dihydroindol-7-yl]ethyl]benzoic acid	KI	2 nM	US-9546162: Compounds and methods for skin repair
2-[[6-[[[4-(3-methylphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	2.2 nM	US-9676720: Substituted biaryl compound
2-[[6-[[[4-(2-ethoxyphenyl)phenyl]methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	2.6 nM	US-9676720: Substituted biaryl compound
5-(furan-3-yl)-3-(4-hydroxyphenyl)-1H-pyrrole-2-carboxylic acid	KI	2.8 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[2,4-difluoro-3-[[3-fluoro-5-(3-fluorophenyl)-2-methylphenyl]methylamino]phenoxy]acetic acid	EC50	3 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[4-fluoro-3-[[3-(3-fluorophenyl)-5-methylphenyl]methylamino]-2-methylphenoxy]acetic acid	EC50	3 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[3-[[2-fluoro-3-(3-fluorophenyl)-5-methylphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	3 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[3-[[3-(3-fluorophenyl)-5-methoxyphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	3 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
2-[3-[[3-fluoro-5-(3-fluorophenyl)-2-methylphenyl]methylamino]-2,4-dimethylphenoxy]acetic acid	EC50	3 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
N-[5-(hydroxycarbamoyl)furan-2-yl]-3-(4-methoxyphenyl)-5-phenyl-1H-pyrrole-2-carboxamide	KI	3.1 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[[6-[[benzenesulfonyl-[[4-(2-ethoxy-4-pyridinyl)phenyl]methyl]amino]methyl]-2-pyridinyl]amino]acetic acid	KI	3.2 nM	US-9676720: Substituted biaryl compound
methyl 6-[[[3-(4-fluorophenyl)-5-thiophen-2-yl-1H-pyrrole-2-carbonyl]amino]methyl]pyridine-3-carboxylate	KI	3.8 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[[6-[[(4-phenylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	3.8 nM	US-9676720: Substituted biaryl compound
2-[3-[[3-carbamoyl-5-(3-fluorophenyl)phenyl]methylamino]-2,4-difluorophenoxy]acetic acid	EC50	4 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application
5-(furan-3-yl)-N-[[4-(hydroxycarbamoyl)phenyl]methyl]-3-(4-hydroxyphenyl)-1H-pyrrole-2-carboxamide	KI	4.4 nM	US-8685986: Medical composition for treatment or prophylaxis of glaucoma
2-[[6-[[[4-(4-fluorophenyl)phenyl]methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	KI	4.4 nM	US-9676720: Substituted biaryl compound
(Z)-7-[(1R,4S,5R)-4-hydroxy-5-[(E,3S)-3-hydroxyoct-1-enyl]-3,3-dimethyl-2-oxocyclopentyl]hept-5-enoic acid	EC50	4.6 nM	US-9156810: Treatment of inflammatory bowel disease
2-[4-fluoro-3-[[5-(3-fluorophenyl)-2-methoxy-3-methylphenyl]methylamino]-2-methylphenoxy]acetic acid	EC50	5 nM	US-9249085: Aniline derivatives, their preparation and their therapeutic application

ChEMBL bioactivities

888 potent at pChembl≥5 of 964 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.17	EC50	0.068	nM	CHEMBL4217198
10.07	EC50	0.086	nM	CHEMBL4204996
9.96	EC50	0.11	nM	CHEMBL3794302
9.96	EC50	0.11	nM	CHEMBL4205480
9.85	EC50	0.14	nM	CHEMBL3793515
9.82	EC50	0.15	nM	CHEMBL3971632
9.82	EC50	0.15	nM	CHEMBL3977724
9.77	EC50	0.17	nM	CHEMBL3794016
9.70	EC50	0.2	nM	CHEMBL3793862
9.68	EC50	0.21	nM	CHEMBL3792632
9.52	Ki	0.3	nM	CHEMBL5966738
9.43	EC50	0.37	nM	CHEMBL4212770
9.41	EC50	0.39	nM	CHEMBL3754586
9.32	EC50	0.48	nM	CHEMBL4206444
9.30	EC50	0.5	nM	CHEMBL3806284
9.28	Ki	0.53	nM	CHEMBL5765756
9.24	EC50	0.57	nM	CHEMBL3793802
9.22	EC50	0.6	nM	CHEMBL3947001
9.21	Ki	0.61	nM	CHEMBL5866875
9.20	Ki	0.63	nM	CHEMBL5285583
9.17	EC50	0.68	nM	CHEMBL3794466
9.17	EC50	0.67	nM	CHEMBL3751951
9.16	EC50	0.69	nM	CHEMBL3793892
9.13	Ki	0.74	nM	CHEMBL64246
9.12	Ki	0.75	nM	CHEMBL6057241
9.12	Ki	0.75	nM	CHEMBL6029044
9.10	Ki	0.8	nM	CHEMBL5936904
9.10	Ki	0.8	nM	CHEMBL5863067
9.10	Ki	0.79	nM	CHEMBL5795595
9.05	EC50	0.9	nM	CHEMBL3793045
9.05	EC50	0.9	nM	CHEMBL3805981
9.05	EC50	0.9	nM	CHEMBL3961932
9.05	Ki	0.9	nM	CHEMBL5899495
9.04	EC50	0.91	nM	CHEMBL3752377
9.03	Ki	0.94	nM	CHEMBL5863530
9.02	Ki	0.95	nM	CHEMBL6063923
9.01	Ki	0.97	nM	CHEMBL5804201
9.00	EC50	1	nM	CHEMBL3903635
9.00	Ki	0.99	nM	CHEMBL6039489
8.99	Ki	1.03	nM	DINOPROSTONE
8.96	Ki	1.1	nM	CHEMBL3670659
8.96	EC50	1.1	nM	CHEMBL4208379
8.96	EC50	1.1	nM	OMIDENEPAG
8.96	EC50	1.1	nM	OMIDENEPAG ISOPROPYL
8.96	Ki	1.1	nM	CHEMBL5853882
8.92	Ki	1.2	nM	CHEMBL6015598
8.85	EC50	1.4	nM	CHEMBL3806130
8.85	Ki	1.4	nM	CHEMBL5799903
8.85	Ki	1.4	nM	CHEMBL5970631
8.82	EC50	1.5	nM	CHEMBL3892847

PubChem BioAssay actives

458 with measured affinity, of 1179 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
2-[(2R,4aR,5S,6R,7aS)-5-[[4-chloro-3-(trifluoromethyl)phenoxy]methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0001	uM
2-[(2R,4aR,5S,6S,7aS)-5-[(4-chloro-3-methylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0001	uM
2-[2-[(1R,2R)-2-[(E,4S)-4-hydroxy-4-methyloct-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0001	uM
2-[2-[(1R,2R)-2-[(E,4S)-8-fluoro-4-hydroxy-4-methyloct-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0001	uM
2-[2-[(1R,2R)-2-[(E,4S)-4-hydroxy-4-methylnon-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0001	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[(2,3,4-trichlorophenoxy)methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0002	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3,5-dimethylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0002	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[(2,4,5-trichlorophenoxy)methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0002	uM
2-[2-[(2R)-2-[(E,3S,5S)-3-hydroxy-5-methylnon-1-enyl]-5-oxopyrrolidin-1-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1272268: Agonist activity at human EP2 receptor	ec50	0.0004	uM
2-[2-[(1R,5R)-2-oxo-5-[(E,4S)-7,7,7-trifluoro-4-hydroxy-4-methylhept-1-enyl]cyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0004	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[[2-(trifluoromethyl)phenoxy]methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0005	uM
2-[2-[(1R,2R)-2-[(E)-4-hydroxy-4-methylnon-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0005	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(3,4-dichlorophenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0006	uM
3-[[4-(4-cyanophenyl)phenoxy]methyl]-1-(4-methoxybenzoyl)pyrrolidine-3-carboxylic acid	1921063: Binding affinity to EP2 receptor in human mast cell assessed as inhibition constant	ki	0.0006	uM
2-[2-[(4S)-4-[(E,3R)-3-[1-(4-fluorobutyl)cyclobutyl]-3-hydroxyprop-1-enyl]-2-oxo-1,3-oxazolidin-3-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0007	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3-methylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0007	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3-ethylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0007	uM
(Z)-7-[(1R,2R,3R,5R)-5-chloro-2-[(E,4S)-4-(1-ethylcyclobutyl)-4-hydroxybut-1-enyl]-3-hydroxycyclopentyl]hept-5-enoic acid	161045: Compound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor	ki	0.0007	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[[3-(trifluoromethyl)phenoxy]methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0009	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[[3-(trifluoromethoxy)phenoxy]methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0009	uM
2-[2-[(2R)-2-[(E,3R)-3-hydroxy-4,4-dimethyloct-1-enyl]-5-oxopyrrolidin-1-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1272268: Agonist activity at human EP2 receptor	ec50	0.0009	uM
dinoprostone	1587869: Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method	ki	0.0010	uM
2-[2-[(1R,2R)-2-[(E,4S)-5-cyclopentyl-4-hydroxy-4-methylpent-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0011	uM
Omidenepag	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0011	uM
omidenepag isopropyl	2129045: Agonist activity at human EP2 receptor expressed in HEK293 cells	ec50	0.0011	uM
2-[(2R,4aR,5R,6R,7aS)-6-hydroxy-5-(2-phenoxyethyl)-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0014	uM
2-[[6-[[(4-pyridin-2-ylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0016	uM
(Z)-7-[(1R,2R,3R,5R)-5-chloro-3-hydroxy-2-[(E,4S)-4-hydroxy-4-(1-prop-2-enylcyclobutyl)but-1-enyl]cyclopentyl]hept-5-enoic acid	1151359: Binding affinity to EP2 receptor (unknown origin) by competitive binding assay	ki	0.0017	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3-methoxyphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0018	uM
4-[[(3R)-9-chloro-7-(5-fluoroindol-1-yl)-3-methyl-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]methyl]-1H-pyridin-2-one	1230408: Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay	ic50	0.0020	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3-propan-2-ylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0020	uM
2-[2-[(1R,2R)-2-[(E,4R)-5-cyclopentyl-4-hydroxy-4-methylpent-1-enyl]-5-oxocyclopentyl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0020	uM
2-[[6-[[(4-phenylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0020	uM
2-[2-[(4S)-4-[(E)-4-hydroxy-4-methylnon-1-enyl]-2-oxo-1,3-oxazolidin-3-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1372357: Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA	ec50	0.0021	uM
5-[(2R,4aR,5S,6R,7aS)-5-[(4-chloro-3-methylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]furan-2-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0022	uM
2-[[6-[[[4-(1-methylcyclopropyl)phenyl]methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0026	uM
2-[[6-[[(4-tert-butylphenyl)methyl-(4-fluorophenyl)sulfonylamino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0027	uM
2-[[6-[[(4-tert-butylphenyl)methyl-pyridin-2-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0027	uM
2-[3-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]phenoxy]acetic acid	1151368: Agonist activity at EP2 receptor (unknown origin) by functional assay	ec50	0.0028	uM
2-[[6-[[(4-tert-butylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0028	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(3,4-dimethylphenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0029	uM
2-[2-[(4S)-4-[(E,3R)-3-(1-butylcyclobutyl)-3-hydroxyprop-1-enyl]-2-oxo-1,3-oxazolidin-3-yl]ethylsulfanyl]-1,3-thiazole-4-carboxylic acid	1272268: Agonist activity at human EP2 receptor	ec50	0.0029	uM
4-[2-[(2R)-2-[(E,3S)-3-(1-butylcyclobutyl)-3-hydroxyprop-1-enyl]-5-oxopyrrolidin-1-yl]ethyl]benzoic acid	320752: Agonist activity at human EP2 receptor by cAMP assay	ec50	0.0030	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(2-chlorophenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0033	uM
2-[[6-[[1-benzothiophen-2-ylmethyl(pyridin-3-ylsulfonyl)amino]methyl]-2-pyridinyl]amino]acetic acid;hydrochloride	1529426: Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins	ec50	0.0034	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[(3-methylphenoxy)methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0036	uM
2-[(2R,4aR,5R,6R,7aS)-6-hydroxy-5-[(E)-3-phenoxyprop-1-enyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0038	uM
2-[(2R,4aR,5S,6R,7aS)-6-hydroxy-5-[[3-methyl-4-(trifluoromethyl)phenoxy]methyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0039	uM
2-[(2R,4aR,5S,6R,7aS)-5-[(4-chlorophenoxy)methyl]-6-hydroxy-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1294757: Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay	ec50	0.0039	uM
2-[(2R,4aR,5R,6R,7aS)-6-hydroxy-5-[(E)-4-phenoxybut-1-enyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300192: Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method	ec50	0.0039	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Dinoprostone	decreases reaction, increases expression, increases activity, increases chemical synthesis, increases response to substance (+4 more)	7
Particulate Matter	decreases expression, increases abundance	3
(+)-JQ1 compound	increases expression, decreases expression	2
Air Pollutants	decreases expression, increases abundance	2
Benzene	increases expression	2
Benzo(a)pyrene	affects methylation, increases expression, increases methylation	2
Diethylhexyl Phthalate	decreases expression, affects cotreatment, affects expression, affects reaction	2
Indomethacin	decreases expression, affects cotreatment	2
Nickel	increases expression	2
Progesterone	decreases expression, increases expression	2
aristolochic acid I	decreases expression	1
3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide	decreases expression	1
ethylbenzene	increases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
diethyl phthalate	affects cotreatment, affects expression, affects reaction	1
testosterone undecanoate	affects cotreatment, decreases expression	1
2-methyl-4-isothiazolin-3-one	increases expression	1
diisononyl phthalate	affects reaction, affects cotreatment, affects expression	1
terbufos	increases methylation	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
sodium arsenite	decreases expression	1
diisobutyl phthalate	affects cotreatment, affects expression, affects reaction	1
2-xylene	increases expression	1
butylbenzyl phthalate	affects cotreatment, affects expression, affects reaction	1
nickel sulfate	increases activity, increases response to substance, increases secretion, increases chemical synthesis, increases reaction	1
cryptotanshinone	decreases reaction, increases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases reaction, increases expression, decreases expression	1
AH 23848	affects binding, affects cotreatment, decreases reaction	1

ChEMBL screening assays

219 unique, capped per target: 162 binding, 57 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009657	Binding	Inhibition of EP2 receptor	Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. — Bioorg Med Chem Lett
CHEMBL1047105	Functional	Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production	Discovery and optimization of CRTH2 and DP dual antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

9 cell lines: 4 transformed cell line, 3 spontaneously immortalized cell line, 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0TL	ACTOne PTGER2	Transformed cell line	Female
CVCL_D8U7	Ubigene HCT 116 PTGER2 KO	Cancer cell line	Male
CVCL_D9Q0	Ubigene HEK293 PTGER2 KO	Transformed cell line	Female
CVCL_H428	CHO-K1/EP2/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV93	cAMP Hunter DLD1 PTGER2 Gs	Cancer cell line	Male
CVCL_KY87	PathHunter CHO-K1 PTGER2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_KZ62	PathHunter HEK 293 PTGER2 beta-arrestin	Transformed cell line	Female
CVCL_YK19	HEK293 PTGER2 HiTSeeker	Transformed cell line	Female
CVCL_ZK81	GeneBLAzer PTGER2-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT01681615	Not specified	UNKNOWN	Challenge Test for Acetylsalicylic Acid Hypersensitivity
NCT02064738	Not specified	COMPLETED	High Omega-3/Low Omega-6 Treatment Diet for Aspirin-exacerbated Respiratory Disease (AERD)