PTGER1

Summary

PTGER1 (prostaglandin E receptor 1, HGNC:9593) is a protein-coding gene on chromosome 19p13.12, encoding Prostaglandin E2 receptor EP1 subtype (P34995). Receptor for prostaglandin E2 (PGE2).

The protein encoded by this gene is a member of the G protein-coupled receptor family. This protein is one of four receptors identified for prostaglandin E2 (PGE2). Through a phosphatidylinositol-calcium second messenger system, G-Q proteins mediate this receptor’s activity. Knockout studies in mice suggested a role of this receptor in mediating algesia and in regulation of blood pressure. Studies in mice also suggested that this gene may mediate adrenocorticotropic hormone response to bacterial endotoxin.

Source: NCBI Gene 5731 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 79 total
• Druggable target: yes — 7 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000955

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9593
Approved symbol	PTGER1
Name	prostaglandin E receptor 1
Location	19p13.12
Locus type	gene with protein product
Status	Approved
Aliases	EP1
Ensembl gene	ENSG00000160951
Ensembl biotype	protein_coding
OMIM	176802
Entrez	5731

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 4 protein_coding

ENST00000292513, ENST00000883541, ENST00000883542, ENST00000947755

RefSeq mRNA: 1 — MANE Select: NM_000955 NM_000955

CCDS: CCDS12309

Canonical transcript exons

ENST00000292513 — 3 exons

Exon	Start	End
ENSE00001055620	14472466	14472826
ENSE00001055622	14473379	14474337
ENSE00001367746	14475262	14475354

Expression profiles

Bgee: expression breadth ubiquitous, 143 present calls, max score 78.67.

FANTOM5 (CAGE): breadth broad, TPM avg 0.5282 / max 48.3036, expressed in 237 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
179642	0.5282	237

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
metanephros cortex	UBERON:0010533	78.67	gold quality
adult mammalian kidney	UBERON:0000082	75.44	gold quality
metanephros	UBERON:0000081	72.49	gold quality
nephron tubule	UBERON:0001231	72.45	silver quality
mucosa of stomach	UBERON:0001199	72.33	gold quality
kidney	UBERON:0002113	71.64	gold quality
triceps brachii	UBERON:0001509	70.88	gold quality
gluteal muscle	UBERON:0002000	70.77	gold quality
spleen	UBERON:0002106	70.15	gold quality
kidney epithelium	UBERON:0004819	69.77	silver quality
pancreatic ductal cell	CL:0002079	68.84	silver quality
metanephric glomerulus	UBERON:0004736	65.78	silver quality
renal glomerulus	UBERON:0000074	65.49	silver quality
body of stomach	UBERON:0001161	65.44	gold quality
cortex of kidney	UBERON:0001225	65.40	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	62.82	gold quality
left adrenal gland cortex	UBERON:0035825	62.74	gold quality
renal medulla	UBERON:0000362	62.68	silver quality
left adrenal gland	UBERON:0001234	62.40	gold quality
stomach	UBERON:0000945	62.39	gold quality
right adrenal gland cortex	UBERON:0035827	62.25	gold quality
right adrenal gland	UBERON:0001233	62.22	gold quality
inferior olivary complex	UBERON:0002127	62.10	gold quality
adrenal cortex	UBERON:0001235	61.07	gold quality
stromal cell of endometrium	CL:0002255	60.42	gold quality
fundus of stomach	UBERON:0001160	60.39	gold quality
upper lobe of left lung	UBERON:0008952	59.67	gold quality
colonic mucosa	UBERON:0000317	59.52	gold quality
nasal cavity epithelium	UBERON:0005384	59.50	gold quality
adult organism	UBERON:0007023	59.50	silver quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.92

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): HIF1A, IRX1

Literature-anchored findings (GeneRIF, showing 37)

• Functional analysis of the mouse counterpart. (PMID:1160156)
• Functional analysis of the mouse counterpart. (PMID:12642666)
• 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)
• the combined effects of EP(1) and EP(4) antagonists on spontaneous polyp formation in APC knockout mice (PMID:12841871)
• Human corpus cavernosum and cultured smooth muscle cells express EP1, EP2 and EP3 receptors. (PMID:14562138)
• COX-2 up-regulates VEGF-C and promotes lymphangiogenesis in human lung adenocarcinoma via the EP(1)/Src/HER-2/Neu signaling pathway. (PMID:14744769)
• PGE2 stimulates extravillous trophoblast migration by signaling through EP1 receptors, increasing [Ca2+]i, and activating calpain (PMID:15886234)
• EP1 receptor level increase in sensory neurones, and macrophage infiltration, appears to precede increased Cox-2 expression by macrophages in nerve injury (PMID:16393343)
• EP(1) does not appear to have a significant direct effect on airway tone but acts as a modulator of the beta(2)AR, altering G(alphas) coupling via steric interactions imposed by the EP(1):beta(2)AR heterodimeric signaling complex (PMID:16670773)
• participates in placentation through EVT invasion by up-regulating PGE2 production and PGE2 receptor expression in first trimester extravillous trophoblasts (PMID:17525067)
• 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)
• Expression of EP1 is frequently seen in human breast cancers. Nuclear expression of EP1 correlates with good prognosis markers like node negative status and progesterone receptor expression. (PMID:17906615)
• Of the 4 EP receptor subtypes, smooth muscle cells in the human pulmonary vein express the EP4 and EP1 receptor subtypes (PMID:18516068)
• The EP1 subtype of prostaglandin E2 receptor has a role in keratinocyte differentiation and expression in non-melanoma skin cancer. (PMID:19625175)
• Prostaglandin E2 enhances the migration of chondrosarcoma cells by increasing alpha2beta1 integrin expression through the EP1/PLC/PKCalpha/c-Src/NF-kappaB signal transduction pathway. (PMID:20178602)
• the PGE(2) and EP1 interaction enhanced migration of oral cancer cells through an increase in ICAM-1 production (PMID:20647315)
• EP1 functions as a suppressor of tumor metastasis; loss of nuclear EP1 is associated with poorer overall survival and may contribute to disparities in outcome in different populations. (PMID:20858737)
• We could not find an association of EP1 gene with suicide in the Japanese population (PMID:21447366)
• Data indicate that not only Cox-2 but also EP1 and EP3 could be important targets for chemosensitization and inhibition of metastasis in breast cancers that are resistant to chemotherapy. (PMID:21813027)
• A novel dendritic cell(DC) progenitor regulatory pathway in which PGE(2) signaling through EP1/EP3 receptors regulates Flt3 expression and downstream STAT3 activation and survivin expression, required for optimal progenitor survival and differentiation. (PMID:22110249)
• The roles of prostaglandin EP 1 and 3 receptors in the control of human myometrial contractility. (PMID:22162473)
• Neuroblastoma express all four forms of PGE(2) receptors. (PMID:22276108)
• new role for the EP(1) receptor in resolving inflammation through down-regulation of COX-2. (PMID:22474323)
• Suggest that the anti-carcinogenic effects of EGCG in hepatocellular carcinoma might be mediated, at least partially, through the suppressing EP(1) receptor expression and PGE(2) production. (PMID:22555372)
• PGE(2) -mediated NF-kappaB activation by simultaneous stimulation of EP(1) and EP(4) receptors induces maximal IL-8 promoter activation and IL-8 mRNA and protein induction (PMID:22924768)
• PGE2-enhanced MMP2 expression is mediated through EP1 receptors and calcium signaling pathway-induced CREB phosphorylation in human cholangiocarcinoma cells. (PMID:23494562)
• Our study suggests that the PGE EP1 receptor regulates FAK phosphorylation by activating the PKC/c-Src and EGFR signal pathways, which may coordinately regulate adhesion and migration in HCC (PMID:23525457)
• through complex formation with D1, EP1 signaling directs the D1 receptor through G(betagamma) to be coupled to AC7. (PMID:23842570)
• COX-1, H446K’ is significantly more sensitive to downregulation by EP . Together these data suggest that distinctive ubiquitination of COX-1 and COX-2 may be responsible for their different sensitivity to EP -mediated degradation. (PMID:24333447)
• A transient interaction between COX-2 and EP1 constitutes a feedback loop whereby an increase in COX-2 expression elevates EP1. (PMID:24614038)
• NF-kappaB inhibitor suppressed 17-PT-PGE2-mediated FoxC2 upregulation. Immunohistochemistry showed p65, FoxC2, EP1 receptor and beta1-integrin were all highly expressed in the HCC cases (PMID:25289898)
• suppression of EP1 prevented RAMA-induced FasL suppression in CLT85 cells at both the mRNA and protein levels (PMID:26211005)
• Copy number variation in PTGER1 is associated with NSAIDs-induced urticaria and/or angioedema (PMID:26959713)
• COX-2 expression appears to be linked to early hepatocellular carcinoma events (initiation), while EP1 receptor expression may participate in tumor progression and predict survival (PMID:27818595)
• No significant differences in EP1 intensity were detected for histological, stage, grading, metastatic and recurrent subtypes in endometrial cancer. (PMID:29134301)
• Prostaglandin E2 EP receptors in cardiovascular disease: An update. (PMID:34822808)
• Impact of Bone Morphogenetic Protein 7 and Prostaglandin receptors on osteoblast healing and organization of collagen. (PMID:38753641)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ptger1c	ENSDARG00000078602
mus_musculus	Ptger1	ENSMUSG00000019464
rattus_norvegicus	Ptger1	ENSRNOG00000004094
drosophila_melanogaster	CG7497	FBGN0036742

Paralogs (7): TBXA2R (ENSG00000006638), PTGER3 (ENSG00000050628), PTGFR (ENSG00000122420), PTGER2 (ENSG00000125384), PTGIR (ENSG00000160013), PTGDR (ENSG00000168229), PTGER4 (ENSG00000171522)

Protein

Protein identifiers

Prostaglandin E2 receptor EP1 subtype — P34995 (reviewed: P34995)

Alternative names: Prostanoid EP1 receptor

All UniProt accessions (1): P34995

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an important modulator of renal function. Implicated the smooth muscle contractile response to PGE2 in various tissues.

Subcellular location. Cell membrane.

Tissue specificity. Abundant in kidney. Lower level expression in lung, skeletal muscle and spleen, lowest expression in testis and not detected in liver brain and heart.

Post-translational modifications. Phosphorylated.

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

RefSeq proteins (1): NP_000946* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000708	Prostglndn_EP1_rcpt	Family
IPR001244	Prostglndn_DP_rcpt	Family
IPR008365	Prostanoid_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (24 total): topological domain 8, transmembrane region 7, sequence variant 3, glycosylation site 2, chain 1, region of interest 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
9M1H	ELECTRON MICROSCOPY	2.55

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P34995-F1	75.11	0.40

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): 110–188

Glycosylation sites (2): 8, 25

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-391908	Prostanoid ligand receptors
R-HSA-416476	G alpha (q) signalling events

MSigDB gene sets: 118 (showing top): GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_RESPONSE_TO_PROSTAGLANDIN_E, GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GGGTGGRR_PAX4_03, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, BROWNE_HCMV_INFECTION_48HR_DN, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, MODULE_289, GOBP_RESPONSE_TO_PROSTAGLANDIN, GOBP_RESPONSE_TO_KETONE, HEN1_01, BROWNE_HCMV_INFECTION_14HR_DN

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), adenylate cyclase-activating dopamine receptor signaling pathway (GO:0007191), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), response to lipopolysaccharide (GO:0032496), response to prostaglandin E (GO:0034695), signal transduction (GO:0007165), phospholipase C-activating G protein-coupled glutamate receptor signaling pathway (GO:0007206)

GO Molecular Function (4): prostaglandin E receptor activity (GO:0004957), D1 dopamine receptor binding (GO:0031748), G protein-coupled receptor activity (GO:0004930), prostaglandin receptor activity (GO:0004955)

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
G protein-coupled receptor signaling pathway	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
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
G protein-coupled dopamine receptor signaling pathway	1
phospholipase C activator activity	1
regulation of biological quality	1
response to molecule of bacterial origin	1
response to lipid	1
response to oxygen-containing compound	1
response to prostaglandin	1
response to alcohol	1
response to ketone	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
PLC activating G protein-coupled glutamate receptor activity	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
G protein-coupled glutamate receptor signaling pathway	1
prostaglandin receptor activity	1
dopamine receptor binding	1
transmembrane signaling receptor activity	1
prostanoid receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

940 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PTGER1	PTGER4	P35408	976
PTGER1	GNAQ	P50148	906
PTGER1	PTGES	O14684	713
PTGER1	PTGS1	P23219	711
PTGER1	PTGES2	Q9H7Z7	703
PTGER1	PTGS2	P35354	660
PTGER1	ZFP3	Q96NJ6	596
PTGER1	ADRB2	P07550	573
PTGER1	PTGES3	Q15185	570
PTGER1	IL1B	P01584	563
PTGER1	PTGER3	P43115	559
PTGER1	TAC1	P20366	510
PTGER1	HPGD	P15428	507
PTGER1	PRKACA	P17612	507
PTGER1	PRKACG	P22612	507

IntAct

5 interactions, top by confidence:

A	B	Type	Score
PTGER1	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
PTGER1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	PTGER1	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	PTGER1	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (4): PTGER1 (Affinity Capture-Western), PTGER1 (Affinity Capture-MS), PTGER1 (Positive Genetic), PTGER1 (FRET)

ESM2 similar proteins: A0A287A2K5, A5A4K9, A5A4L1, O08725, O43193, O54897, O77808, O88721, P30518, P30552, P30553, P30796, P30937, P31391, P32239, P32307, P32745, P34995, P35346, P35375, P41231, P46095, P46627, P48044, P48748, P49220, P49660, P51651, P56481, P79266, Q00788, Q15722, Q684M3, Q6YNI2, Q8HYC3, Q8HZN9, Q8HZP1, Q8MJV3, Q91X56, Q92847

Diamond homologs: O02662, P21731, P30557, P30987, P34978, P34979, P34980, P34995, P35375, P37289, P43088, P43115, P43117, P43118, P43119, P43141, P43252, P43253, P46069, P46626, P50131, P56486, P70597, P79393, Q28524, Q28550, Q28905, Q804Q2, Q804X9, Q8R456, Q95125, Q95252, Q9BGL8, Q9QXZ9, Q9TST4, Q9UHM6, Q9XT57, Q9XT58, P32240, P35408

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
PTGER1	up-regulates	GNAQ	binding
PTGER1	“up-regulates activity”	GNAS	binding
PTGER1	“up-regulates activity”	GNAL	binding
PTGER1	“up-regulates activity”	GNAQ	binding
PTGER1	“up-regulates activity”	GNA14	binding
PTGER1	“up-regulates activity”	GNA12	binding
“prostaglandin E2(1-)”	“up-regulates activity”	PTGER1	“chemical activation”
IRX1	“down-regulates quantity by repression”	PTGER1	“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	72
Likely benign	5
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

252 predictions. Top by Δscore:

Variant	Effect	Δscore
19:14473408:C:CT	donor_gain	0.9900
19:14474338:C:CC	acceptor_gain	0.9900
19:14475256:CCTTA:C	donor_loss	0.9900
19:14475257:CTTAC:C	donor_loss	0.9900
19:14475258:TTACC:T	donor_loss	0.9900
19:14475259:TAC:T	donor_loss	0.9900
19:14475260:AC:A	donor_gain	0.9900
19:14475260:ACCC:A	donor_loss	0.9900
19:14475261:C:CT	donor_loss	0.9900
19:14475261:CC:C	donor_gain	0.9900
19:14475270:G:GA	donor_gain	0.9900
19:14473409:C:CT	donor_gain	0.9800
19:14474334:GGTG:G	acceptor_gain	0.9800
19:14474335:GTG:G	acceptor_gain	0.9800
19:14474336:TG:T	acceptor_gain	0.9800
19:14474336:TGCTG:T	acceptor_loss	0.9800
19:14474337:GCTG:G	acceptor_loss	0.9800
19:14474338:C:G	acceptor_loss	0.9800
19:14474339:T:A	acceptor_loss	0.9800
19:14474342:A:AC	acceptor_gain	0.9800
19:14475260:A:AC	donor_gain	0.9800
19:14475261:C:CC	donor_gain	0.9800
19:14475261:CCCGG:C	donor_gain	0.9800
19:14472825:ACCT:A	acceptor_loss	0.9700
19:14472826:CCT:C	acceptor_loss	0.9700
19:14472827:C:A	acceptor_loss	0.9700
19:14472828:T:A	acceptor_loss	0.9700
19:14473423:CAAG:C	donor_gain	0.9700
19:14474333:GGGTG:G	acceptor_gain	0.9700
19:14472824:CAC:C	acceptor_gain	0.9600

AlphaMissense

2475 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:14473388:G:C	S311R	0.997
19:14473388:G:T	S311R	0.997
19:14473390:T:G	S311R	0.997
19:14472724:A:G	W349R	0.996
19:14472724:A:T	W349R	0.996
19:14472740:G:C	N343K	0.995
19:14472740:G:T	N343K	0.995
19:14472726:G:T	P348H	0.994
19:14473754:G:C	F189L	0.994
19:14473754:G:T	F189L	0.994
19:14473756:A:G	F189L	0.994
19:14473395:C:T	C309Y	0.993
19:14473655:G:C	N222K	0.993
19:14473655:G:T	N222K	0.993
19:14473760:C:A	W187C	0.993
19:14473760:C:G	W187C	0.993
19:14474171:G:C	N50K	0.993
19:14474171:G:T	N50K	0.993
19:14474185:C:G	G46R	0.993
19:14473394:G:C	C309W	0.992
19:14473396:A:G	C309R	0.992
19:14472745:A:G	W342R	0.991
19:14472745:A:T	W342R	0.991
19:14473393:A:G	W310R	0.991
19:14473393:A:T	W310R	0.991
19:14473762:A:G	W187R	0.991
19:14473762:A:T	W187R	0.991
19:14474102:G:C	F73L	0.990
19:14474102:G:T	F73L	0.990
19:14474104:A:G	F73L	0.990

dbSNP variants (sampled 300 via entrez): RS1000728500 (19:14475447 G>A), RS1000738273 (19:14475634 T>C), RS1001895499 (19:14475048 C>T), RS1002605559 (19:14472361 C>A,T), RS1003137970 (19:14475696 T>G), RS1003520629 (19:14473161 A>C), RS1003613932 (19:14473467 G>A), RS1003836132 (19:14472791 A>C,G), RS1003964033 (19:14477229 C>T), RS1004044735 (19:14474462 A>G), RS1004481673 (19:14474241 G>A,C,T), RS1004695989 (19:14472885 T>A,C), RS1005578201 (19:14475910 C>A,G,T), RS1006052837 (19:14476369 C>T), RS1006453299 (19:14472102 A>C)

Disease associations

OMIM: gene MIM:176802 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1811 (SINGLE PROTEIN), CHEMBL2363068 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

7 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 19,858 (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
CHEMBL494	ILOPROST	4	234
CHEMBL548	DINOPROSTONE	4	14,939
CHEMBL815	DINOPROST	4	3,118
CHEMBL3301604	RALINEPAG	3	260
CHEMBL2220404	CLOPROSTENOL	2

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 (28 total), top 25:

Ligand	Action	Affinity	Parameter
ONO-8711	Antagonist	9.2	pKi
GW848687X	Antagonist	8.6	pIC50
MF266-1	Antagonist	8.44	pKi
17-phenyl-ω-trinor-PGE2	Full agonist	8.1	pKi
ONO-8130	Antagonist	8.03	pIC50
PGE2	Full agonist	8.0	pKi
iloprost	Full agonist	8.0	pKi
ONO-8713	Antagonist	8.0	pKi
[3H]PGE2	Full agonist	7.9	pKd
SC-51322	Antagonist	7.9	pKi
enprostil	Full agonist	7.8	pKi
carbacyclin	Full agonist	7.6	pKi
ZK118182	Partial agonist	7.1	pKi
sulprostone	Full agonist	7.0	pKi
PGE1	Full agonist	6.8	pKi
ONO-DI-004	Full agonist	6.8	pKi
ZK110841	Partial agonist	6.8	pKi
treprostinil	Full agonist	6.7	pKi
MB-28767	Full agonist	6.4	pKi
PGF2α	Full agonist	6.3	pKi
cloprostenol	Full agonist	6.1	pKi
AH6809	Antagonist	6.0	pKi
cicaprost	Full agonist	5.9	pKi
SC-51089	Antagonist	5.9	pKi
PGI2	Full agonist	4.8	pKi

Binding affinities (BindingDB)

18 measured of 35 human assays (36 total across all organisms); most potent 18 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
NSC_5311503	KI	0.3 nM
NSC_3080928	KI	0.4 nM
CAS_41598-07-6	KI	1.7 nM
(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
4-[[6-(4-hydroxypiperidin-1-yl)-3-methylpyridine-2-carbonyl]amino]-3,5-dimethylbenzoic acid	IC50	9.8 nM	US-8933099: Monocyclic pyridine derivative
7-[(1R,4S,5R)-4-hydroxy-5-[(E,3S)-3-hydroxyoct-1-enyl]-3,3-dimethyl-2-oxocyclopentyl]hept-5-ynoic acid	EC50	11 nM	US-9156810: Treatment of inflammatory bowel disease
PGI2	KI	132 nM
(Z)-7-[(1R,4S,5R)-4-hydroxy-5-[(E)-3-hydroxy-4-phenylbut-1-enyl]-3,3-dimethyl-2-oxocyclopentyl]hept-5-enoic acid	EC50	589 nM	US-9156810: Treatment of inflammatory bowel disease
CAS_54751	KI	697 nM
(Z)-7-[(1R,3R,5S)-3,5-Dihydroxy-2-((E)-(S)-3-hydroxy-oct-1-enyl)-cyclopentyl]-hept-5-enoic acid	KI	861 nM
ILOPROST	KI	1040 nM
CAS_94079-80-8	KI	1340 nM
CAS_33458-93-4	KI	1420 nM
(Z)-7-[(1R,4S,5R)-4-hydroxy-5-[(E)-3-hydroxy-5-phenylpent-1-enyl]-3,3-dimethyl-2-oxocyclopentyl]hept-5-enoic acid	EC50	1860 nM	US-9156810: Treatment of inflammatory bowel disease
7-[(1R,4S,5R)-5-[(E)-4-(1-benzothiophen-2-yl)-3-hydroxybut-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxocyclopentyl]hept-5-ynoic acid	IC50	2050 nM	US-9156810: Treatment of inflammatory bowel disease
U46619	KI	3970 nM
(Z)-7-[(1R,4S,5R)-5-[(E)-4-(1-benzothiophen-2-yl)-3-hydroxybut-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxocyclopentyl]hept-5-enoic acid	IC50	4700 nM	US-9156810: Treatment of inflammatory bowel disease
methyl (Z)-7-[(1R,4S,5R)-4-hydroxy-5-[(E)-3-hydroxy-5-phenylpent-1-enyl]-3,3-dimethyl-2-oxocyclopentyl]hept-5-enoate	IC50	6610 nM	US-9156810: Treatment of inflammatory bowel disease

ChEMBL bioactivities

917 potent at pChembl≥5 of 967 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.20	Ki	0.0631	nM	CHEMBL402392
10.00	Ki	0.1	nM	CHEMBL427844
9.89	IC50	0.1288	nM	CHEMBL2110364
9.88	IC50	0.1318	nM	CHEMBL214971
9.70	Ki	0.1995	nM	CHEMBL257134
9.52	Ki	0.3	nM	CHEMBL362543
9.52	IC50	0.3	nM	CHEMBL4129609
9.52	EC50	0.3	nM	ILOPROST
9.51	Ki	0.309	nM	CHEMBL362543
9.50	Ki	0.3162	nM	CHEMBL403330
9.40	IC50	0.3981	nM	CHEMBL387969
9.40	IC50	0.3981	nM	CHEMBL228586
9.40	IC50	0.3981	nM	CHEMBL427844
9.40	Ki	0.3981	nM	CHEMBL1915012
9.35	Ki	0.45	nM	CHEMBL3127163
9.31	Ki	0.4898	nM	CHEMBL214971
9.30	IC50	0.5012	nM	CHEMBL390189
9.30	Ki	0.5012	nM	CHEMBL257997
9.30	Ki	0.5	nM	CHEMBL257997
9.28	IC50	0.5248	nM	CHEMBL214967
9.26	Ki	0.5495	nM	CHEMBL215992
9.23	Ki	0.5888	nM	CHEMBL383090
9.22	IC50	0.6	nM	CHEMBL3127163
9.20	IC50	0.631	nM	CHEMBL387878
9.15	Ki	0.7079	nM	CHEMBL377852
9.15	IC50	0.7	nM	CHEMBL4126319
9.10	IC50	0.7943	nM	CHEMBL228593
9.10	IC50	0.7943	nM	CHEMBL430360
9.10	Kd	0.7943	nM	CHEMBL234940
9.10	Ki	0.7943	nM	CHEMBL270208
9.05	IC50	0.9	nM	CHEMBL3092131
9.00	IC50	1	nM	CHEMBL3127157
9.00	IC50	1	nM	CHEMBL211534
9.00	Ki	1	nM	CHEMBL231184
9.00	Ki	1	nM	CHEMBL402338
8.96	IC50	1.1	nM	CHEMBL3127159
8.96	IC50	1.1	nM	DINOPROSTONE
8.95	Ki	1.122	nM	CHEMBL384332
8.90	Ki	1.259	nM	CHEMBL362543
8.90	IC50	1.259	nM	CHEMBL395248
8.90	IC50	1.259	nM	CHEMBL230765
8.90	IC50	1.259	nM	CHEMBL228963
8.90	IC50	1.259	nM	CHEMBL428367
8.90	IC50	1.259	nM	CHEMBL390238
8.90	IC50	1.259	nM	CHEMBL234727
8.90	IC50	1.259	nM	CHEMBL234519
8.90	Ki	1.259	nM	CHEMBL403407
8.85	EC50	1.4	nM	CHEMBL3804978
8.80	IC50	1.585	nM	CHEMBL210394
8.80	IC50	1.585	nM	CHEMBL234945

PubChem BioAssay actives

955 with measured affinity, of 1433 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
3-acetamido-5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	292922: Inhibition of EP1 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay	ki	0.0001	uM
1-[[5-bromo-2-[(2,4-dichlorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylic acid	270733: Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells	ic50	0.0001	uM
sodium 2-[3-(2-methylpropyl)-6-(trifluoromethyl)indol-1-yl]-1,3-thiazole-4-carboxylate	329792: Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay	ki	0.0001	uM
sodium 1-[[5-bromo-2-[(2,4-dichlorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylate	352440: Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells	ic50	0.0001	uM
sodium 2-[6-bromo-3-(2-methylpropyl)indol-1-yl]-1,3-thiazole-4-carboxylate	329792: Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay	ki	0.0002	uM
sodium 5-[[5-chloro-2-(2-methylpropoxy)phenyl]methyl]furan-2-carboxylate	320100: Antagonist activity at EP1 receptor by FLIPR assay	ki	0.0003	uM
Iloprost	1872475: Agonist activity at human EP1 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ec50	0.0003	uM
2-[3-phenyl-6-(trifluoromethyl)pyrazolo[5,4-b]pyridin-1-yl]-1,3-thiazole-4-carboxylic acid	1498799: Antagonist activity at EP1 receptor (unknown origin) by reporter gene assay	ic50	0.0003	uM
3-[3-(5-chloro-2-phenylmethoxyphenyl)thiophen-2-yl]benzoic acid	264796: Antagonist activity against PGE2 activated EP1 receptor assessed as ability to inhibit intracellular calcium mobilisation by FLIPR	ki	0.0003	uM
5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-methoxybenzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0004	uM
1-[(5-chloro-2-propan-2-yl-1-benzofuran-7-yl)methyl]-5-methylpyrazole-3-carboxylic acid	628032: Antagonist activity at human recombinant EP1 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR method	ki	0.0004	uM
2-acetamido-5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0004	uM
2-[3-phenyl-6-(trifluoromethyl)indazol-1-yl]-1,3-thiazole-4-carboxylic acid	1075941: Binding affinity to human EP1 receptor	ki	0.0004	uM
1-[[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylic acid	270733: Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells	ic50	0.0005	uM
1-[[5-chloro-2-[(2,4-dichlorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylic acid	270731: Antagonist activity at EP1 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-stimulated calcium ion mobilization by FLIPR assay	ki	0.0005	uM
3-amino-5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0005	uM
sodium 2-[6-chloro-3-(2-methylpropyl)indol-1-yl]-1,3-thiazole-4-carboxylate	329792: Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay	ki	0.0005	uM
5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-(difluoromethoxy)benzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0006	uM
3-[2-(5-chloro-2-phenylmethoxyphenyl)pyrrol-1-yl]benzoic acid	264796: Antagonist activity against PGE2 activated EP1 receptor assessed as ability to inhibit intracellular calcium mobilisation by FLIPR	ki	0.0006	uM
3-[2-(5-chloro-2-phenylmethoxyphenyl)-5-methylpyrrol-1-yl]benzoic acid	264796: Antagonist activity against PGE2 activated EP1 receptor assessed as ability to inhibit intracellular calcium mobilisation by FLIPR	ki	0.0007	uM
2-[3-(3,4-dihydro-2H-pyran-6-yl)-6-(trifluoromethyl)indazol-1-yl]-1,3-thiazole-4-carboxylic acid	1498799: Antagonist activity at EP1 receptor (unknown origin) by reporter gene assay	ic50	0.0007	uM
6-[2-[5-chloro-2-[(2,4-difluorophenyl)methoxy]phenyl]cyclopenten-1-yl]pyridine-2-carboxylic acid	292809: Antagonist activity at human EP1 receptor	kd	0.0008	uM
3-amino-5-[2-[5-bromo-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-methylbenzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0008	uM
sodium 1-[[5-chloro-2-(2-methylpropoxy)phenyl]methyl]-5-methylpyrazole-3-carboxylate	320100: Antagonist activity at EP1 receptor by FLIPR assay	ki	0.0008	uM
3-acetamido-5-[2-[5-bromo-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0008	uM
2-(3-phenyl-4H-indeno[2,1-d]pyrazol-1-yl)-1,3-thiazole-4-carboxylic acid	1059344: Antagonist activity human EP1 receptor assessed as inhibition of PGE2-induced effect by reporter gene assay	ic50	0.0009	uM
3-[2-[5-bromo-2-[(2,6-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	268181: Inhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cells	ic50	0.0010	uM
5-[2-[5-chloro-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-methylbenzoic acid	290056: Inhibition of human recombinant EP1 receptor expressed in CHO cells by calcium mobilisation assay	ki	0.0010	uM
sodium 2-[6-chloro-3-(2-methylpropyl)indol-1-yl]-1,3-oxazole-4-carboxylate	329792: Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay	ki	0.0010	uM
2-(6-methyl-3-phenylindazol-1-yl)-1,3-thiazole-4-carboxylic acid	1075944: Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay	ic50	0.0010	uM
1-[[5-chloro-2-[(2,4-difluorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylic acid	270731: Antagonist activity at EP1 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-stimulated calcium ion mobilization by FLIPR assay	ki	0.0011	uM
dinoprostone	482503: Binding affinity to EP1 receptor	ic50	0.0011	uM
2-(6-methoxy-3-phenylindazol-1-yl)-1,3-thiazole-4-carboxylic acid	1075944: Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay	ic50	0.0011	uM
5-[2-[5-bromo-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-fluorobenzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0013	uM
5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-2-methylbenzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0013	uM
6-[2-(5-chloro-2-phenylmethoxyphenyl)-5-methylpyrrol-1-yl]-1H-indole-4-carboxylic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0013	uM
3-acetamido-5-[2-(5-bromo-2-phenylmethoxyphenyl)-5-methylpyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0013	uM
3-acetamido-5-[2-methyl-5-[2-phenylmethoxy-5-(trifluoromethyl)phenyl]pyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0013	uM
3-[acetyl(methyl)amino]-5-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0013	uM
3-[2-[5-bromo-2-[(2,4-difluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-5-(2-oxopiperidin-1-yl)benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0013	uM
sodium 5-[6-chloro-3-(2-methylpropyl)indol-1-yl]furan-2-carboxylate	329792: Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay	ki	0.0013	uM
2-[(2R,4aR,5R,6R,7aS)-6-hydroxy-5-[(E,3R)-3-hydroxy-4-phenoxybut-1-enyl]-2,3,4,4a,5,6,7,7a-octahydrocyclopenta[b]pyran-2-yl]-1,3-thiazole-4-carboxylic acid	1300198: Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis	ec50	0.0014	uM
3-[2-[5-bromo-2-[(2,4,6-trifluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]benzoic acid	268181: Inhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cells	ic50	0.0016	uM
sodium 2-[(5-chloro-2-phenylmethoxyphenyl)methyl]-1,3-oxazole-4-carboxylate	320100: Antagonist activity at EP1 receptor by FLIPR assay	ki	0.0016	uM
3-acetamido-5-[2-[2-[(2,4-difluorophenyl)methoxy]-5-iodophenyl]-5-methylpyrrol-1-yl]benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0016	uM
3-[2-[5-chloro-2-[(4-fluorophenyl)methoxy]phenyl]-5-methylpyrrol-1-yl]-5-(methanesulfonamido)benzoic acid	292911: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes	ic50	0.0016	uM
5-[2-[5-chloro-2-[(4-fluorophenyl)methoxy]phenyl]cyclopenten-1-yl]-2-methylpyridine-3-carboxylic acid	292796: Inhibition of human EP1 receptor	ic50	0.0016	uM
4-[2-(5-chloro-2-phenylmethoxyphenyl)-5-methylpyrrol-1-yl]-N-[(1R)-1-phenylethyl]benzamide	298760: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cells	ic50	0.0016	uM
3-(butanoylamino)-5-[2-(5-chloro-2-phenylmethoxyphenyl)phenyl]benzoic acid	396135: Binding affinity to EP1 receptor	ic50	0.0020	uM
3-amino-5-[2-(5-chloro-2-phenylmethoxyphenyl)-5-methylpyrrol-1-yl]-2-methylbenzoic acid	290042: Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane	ic50	0.0020	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects cotreatment, increases abundance, increases expression	2
Dinoprostone	affects cotreatment, decreases reaction, increases activity, increases reaction, increases expression (+3 more)	2
diethyl phthalate	decreases reaction, affects cotreatment, affects reaction, decreases expression	1
diisononyl phthalate	affects cotreatment, affects reaction, decreases expression, decreases reaction	1
2,4,5,2’,4’,5’-hexachlorobiphenyl	increases expression	1
manganese chloride	increases expression, affects cotreatment, increases abundance	1
diisobutyl phthalate	affects cotreatment, affects reaction, decreases expression, decreases reaction	1
butylbenzyl phthalate	affects reaction, decreases expression, decreases reaction, affects cotreatment	1
puerarin	decreases expression	1
epigallocatechin gallate	decreases expression	1
exoenzyme C3, Clostridium botulinum	increases phosphorylation, affects cotreatment, decreases reaction, increases expression	1
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide	affects cotreatment, decreases reaction, increases expression, increases phosphorylation	1
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	increases reaction, affects binding, increases activity, increases expression	1
CGP 52608	affects binding, increases reaction	1
PCB 180	affects expression	1
3-(4-methylphenylsulfonyl)-2-propenenitrile	affects cotreatment, decreases reaction, increases expression	1
pomiferin	decreases expression	1
osajin	decreases expression	1
rosavin	decreases expression	1
licochalcone B	increases expression	1
Resveratrol	decreases expression	1
Wortmannin	increases activity, increases expression, increases phosphorylation, affects binding, decreases reaction	1
Air Pollutants	decreases expression, increases abundance	1
Arsenic	affects cotreatment, increases abundance, increases expression	1
Benzo(a)pyrene	affects methylation, decreases methylation, increases methylation	1
Dibutyl Phthalate	affects reaction, decreases expression, decreases reaction, affects cotreatment	1
Diethylhexyl Phthalate	decreases expression, decreases reaction, affects cotreatment, affects reaction	1
Hydrocarbons, Fluorinated	affects binding, decreases activity	1
Inositol Phosphates	affects binding, increases abundance, increases activity	1
Manganese	increases abundance, increases expression, affects cotreatment	1

ChEMBL screening assays

168 unique, capped per target: 113 binding, 54 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009645	Functional	Antagonist activity at human recombinant EP1 receptor expressed in CHO cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR method	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
CHEMBL1009646	Binding	Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells	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
CHEMBL4326152	ADMET	Displacement of [3H]prostaglandin E2 from recombinant human full length EP1 receptor expressed in Chem-1 cell membranes after 60 mins by liquid scintillation counting	Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl. — J Med Chem

Cellosaurus cell lines

5 cell lines: 2 spontaneously immortalized cell line, 2 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H366	293/EP1	Transformed cell line	Female
CVCL_KU61	CHO-K1 PTGER1 Gq	Spontaneously immortalized cell line	Female
CVCL_LB18	PathHunter U2OS PTGER1 beta-arrestin	Cancer cell line	Female
CVCL_YK56	U2OS PTGER1 HiTSeeker	Cancer cell line	Female
CVCL_ZK80	GeneBLAzer PTGER1-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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