PTGES2

Summary

PTGES2 (prostaglandin E synthase 2, HGNC:17822) is a protein-coding gene on chromosome 9q34.11, encoding Prostaglandin E synthase 2 (Q9H7Z7). Isomerase that catalyzes the conversion of PGH2 into the more stable prostaglandin E2 (PGE2) (in vitro).

The protein encoded by this gene is a membrane-associated prostaglandin E synthase, which catalyzes the conversion of prostaglandin H2 to prostaglandin E2. This protein also has been shown to activate the transcription regulated by a gamma-interferon-activated transcription element (GATE). Multiple transcript variants have been found for this gene.

Source: NCBI Gene 80142 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 72 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_025072

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17822
Approved symbol	PTGES2
Name	prostaglandin E synthase 2
Location	9q34.11
Locus type	gene with protein product
Status	Approved
Aliases	mPGES-2, FLJ14038
Ensembl gene	ENSG00000148334
Ensembl biotype	protein_coding
OMIM	608152
Entrez	80142

Gene structure

Transcript identifiers

Ensembl transcripts: 25 — 10 protein_coding, 6 nonsense_mediated_decay, 6 retained_intron, 3 protein_coding_CDS_not_defined

ENST00000277462, ENST00000338961, ENST00000449878, ENST00000474124, ENST00000476655, ENST00000476748, ENST00000483625, ENST00000485237, ENST00000485510, ENST00000487063, ENST00000493205, ENST00000496594, ENST00000497109, ENST00000617202, ENST00000676562, ENST00000677651, ENST00000677691, ENST00000677980, ENST00000678174, ENST00000678916, ENST00000679345, ENST00000868346, ENST00000930204, ENST00000930205, ENST00000957708

RefSeq mRNA: 3 — MANE Select: NM_025072 NM_001256335, NM_025072, NM_198938

CCDS: CCDS6891

Canonical transcript exons

ENST00000338961 — 7 exons

Exon	Start	End
ENSE00001390373	128127439	128127729
ENSE00001904963	128120693	128121273
ENSE00003434237	128122362	128122479
ENSE00003467045	128123702	128123851
ENSE00003486911	128122934	128123134
ENSE00003582805	128124492	128124550
ENSE00003691232	128125244	128125441

Expression profiles

Bgee: expression breadth ubiquitous, 271 present calls, max score 98.28.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 23.1780 / max 151.2561, expressed in 1813 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
102656	18.8315	1808
102658	1.6728	889
102659	0.9336	539
102660	0.9069	564
102655	0.4406	250
102654	0.2141	95
102657	0.1785	90

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
apex of heart	UBERON:0002098	98.28	gold quality
gastrocnemius	UBERON:0001388	96.77	gold quality
mucosa of transverse colon	UBERON:0004991	96.13	gold quality
heart left ventricle	UBERON:0002084	96.11	gold quality
right atrium auricular region	UBERON:0006631	96.00	gold quality
muscle of leg	UBERON:0001383	95.90	gold quality
cardiac ventricle	UBERON:0002082	95.86	gold quality
right frontal lobe	UBERON:0002810	95.57	gold quality
prefrontal cortex	UBERON:0000451	95.50	gold quality
anterior cingulate cortex	UBERON:0009835	95.49	gold quality
hindlimb stylopod muscle	UBERON:0004252	95.48	gold quality
cingulate cortex	UBERON:0003027	95.43	gold quality
cardiac atrium	UBERON:0002081	95.26	gold quality
left adrenal gland	UBERON:0001234	95.22	gold quality
right adrenal gland	UBERON:0001233	95.18	gold quality
right adrenal gland cortex	UBERON:0035827	95.13	gold quality
left adrenal gland cortex	UBERON:0035825	95.11	gold quality
adenohypophysis	UBERON:0002196	95.03	gold quality
heart	UBERON:0000948	94.34	gold quality
muscle organ	UBERON:0001630	94.17	gold quality
nucleus accumbens	UBERON:0001882	94.17	gold quality
adrenal cortex	UBERON:0001235	94.13	gold quality
right hemisphere of cerebellum	UBERON:0014890	94.08	gold quality
metanephros cortex	UBERON:0010533	93.89	gold quality
pituitary gland	UBERON:0000007	93.83	gold quality
transverse colon	UBERON:0001157	93.71	gold quality
amygdala	UBERON:0001876	93.68	gold quality
cerebellar cortex	UBERON:0002129	93.66	gold quality
cerebellar hemisphere	UBERON:0002245	93.65	gold quality
putamen	UBERON:0001874	93.60	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.98

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

23 targeting PTGES2, 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-4481	100.00	66.42	1669
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-137-3P	99.87	74.74	2401
HSA-MIR-6842-5P	99.80	67.54	1587
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-6752-5P	99.59	67.32	1243
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-486-3P	99.51	66.82	1901
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-6727-3P	99.49	65.92	1333
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-3152-3P	99.10	66.35	678
HSA-MIR-181A-2-3P	98.91	67.60	1168
HSA-MIR-4763-5P	98.75	63.89	854
HSA-MIR-6509-3P	98.32	67.33	1343
HSA-MIR-1225-3P	97.29	64.60	876

Literature-anchored findings (GeneRIF, showing 16)

• Up-regulation of prostaglandin E2 synthesis by interleukin-1beta in human orbital fibroblasts involves coordinate induction of prostaglandin-endoperoxide H synthase-2 and glutathione-dependent prostaglandin E2 synthase expression (PMID:11847219)
• role in regulating interferon-gamma-dependent gene expression (PMID:12050152)
• 110Cys is essential in the active site of membrane-associated prostaglandin E synthase-2 (PMID:12804604)
• Transactivators GBF1 and CCAAT/enhancer-binding protein-beta physically interact to induce interferon-gamma-regulated transcription; a 37-aa long peptide derived from the GBF1 protein can associate with C/EBP-beta in an IFN-inducible manner. (PMID:15879117)
• alphaTOS inhibits COX activity, thereby inhibiting PGE2 production in human lung epithelial cells (PMID:16714329)
• study obtained evidence from two Caucasian study populations that the His298-allele of PTGES2 Arg298His confers to reduced risk of type 2 diabetes (PMID:17566096)
• Carbonyl reductase-1 (CBR1), microsomal prostaglandin E synthase-1 and 2 (mPGES-1, mPGES-2), cytosolic prostaglandin E synthase (cPGES), aldoketoreductase (AKR1C1) and prostaglandin F synthase (AKR1C3) were all expressed in hair follicles. (PMID:17697149)
• risk-reducing effects of the minor His allele of the prostaglandin E synthase 2 (PTGES2) Arg298His polymorphism could be mediated partly by lowered body mass index (BMI) (PMID:17979097)
• all three terminal prostaglandin synthases, mPGES-1, mPGES-2, and cPGES, are over-expressed in human gliomas (PMID:19347995)
• A marginal but significant influence of the PTGES2 298H single nucleotide polymorphism on BMI was found in a large population-based study. (PMID:19371221)
• These results indicate that mPGES-1 and mPGES-2 may each play a role in colorectal cancer progression. (PMID:19412621)
• high immunoreactivity of mPGES-2 in pyramidal neurons of AD brains indicates that it might have a potential role in the functional replacement of cytosolic PGES or inactive mPGES-1 in later stages of Alzheimer disease (PMID:19664621)
• Four single nucleotide polymorphisms in two genes in the PGE2 family, PTGES2 and PTGER4, were significantly associated with primary graft dysfunction after lung transplantation. (PMID:24467603)
• This suggests that the interaction with the microenvironment occurs at both early and late thyroid tumor stages, and favors tumor progression. The co-expression of PTGS2 gene and M2 markers in human thyroid carcinoma highlights the possibility to counteract tumor growth through COX-2 inhibition. (PMID:31113465)
• Parasitic load determination by differential expressions of 5-lipoxygenase and PGE2 synthases in visceral leishmaniasis. (PMID:31726220)
• Inhibiting cholesterol de novo synthesis promotes hepatocellular carcinoma progression by upregulating prostaglandin E synthase 2-mediated arachidonic acid metabolism under high fatty acid conditions. (PMID:38081591)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	ptgesl	ENSDARG00000068415
mus_musculus	Ptges2	ENSMUSG00000026820
rattus_norvegicus	Ptges2	ENSRNOG00000014050
drosophila_melanogaster	Su(P)	FBGN0004465
caenorhabditis_elegans		WBGENE00011239

Protein

Protein identifiers

Prostaglandin E synthase 2 — Q9H7Z7 (reviewed: Q9H7Z7)

Alternative names: Membrane-associated prostaglandin E synthase-2, Microsomal prostaglandin E synthase 2, Prostaglandin-H(2) E-isomerase

All UniProt accessions (9): Q9H7Z7, A0A7I2V308, A0A7I2V460, A0A7I2V4L3, A0A7I2V5T7, A0A7I2V5X6, A0A7I2YQ70, A6NHH0, X6RJ95

UniProt curated annotations — full annotation on UniProt →

Function. Isomerase that catalyzes the conversion of PGH2 into the more stable prostaglandin E2 (PGE2) (in vitro). The biological function and the GSH-dependent property of PTGES2 is still under debate. In vivo, PTGES2 could form a complex with GSH and heme and would not participate in PGE2 synthesis but would catalyze the degradation of prostaglandin E2 H2 (PGH2) to 12(S)-hydroxy-5(Z),8(E),10(E)-heptadecatrienoic acid (HHT) and malondialdehyde (MDA).

Subunit / interactions. Homodimer. May interact with CEBPB. Interacts with EXOSC10.

Subcellular location. Golgi apparatus membrane Cytoplasm. Perinuclear region.

Tissue specificity. Widely expressed. Expressed in the heart, including apex, inter-ventricular septum, both atria and ventricles, but not in the aorta. Also expressed in fetal heart. Detected in various regions of the brain: cerebellum; occipital, frontal and parietal lobes. Also expressed in the lymph nodes, skeletal muscle, kidney and trachea, but not in the thymus or lung. Overexpressed in colorectal cancer.

Post-translational modifications. Synthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads to the formation of a mature cytosolic enzyme.

Activity regulation. Isomerase activity is increased by sulfhydril compounds. Dithiothreitol (DTT) is most effective, followed by dihydrolipoic acid, glutathione (GSH) and 2-mercaptoethanol.

Pathway. Lipid metabolism; prostaglandin biosynthesis.

Similarity. Belongs to the GST superfamily.

RefSeq proteins (3): NP_001243264, NP_079348, NP_945176 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004045	Glutathione_S-Trfase_N	Domain
IPR010987	Glutathione-S-Trfase_C-like	Domain
IPR034334	PGES2	Family
IPR034335	PGES2_C	Domain
IPR036249	Thioredoxin-like_sf	Homologous_superfamily
IPR036282	Glutathione-S-Trfase_C_sf	Homologous_superfamily
IPR040079	Glutathione_S-Trfase	Family

Pfam: PF13417

Enzyme classification (BRENDA):

• EC 5.3.99.3 — prostaglandin-E synthase (BRENDA: 17 organisms, 30 substrates, 487 inhibitors, 29 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
PROSTAGLANDIN H2	0.0149–0.5345	16
(5Z,13E)-(15S)-9ALPHA,11ALPHA-EPIDIOXY-15-HYDROX	0.0024–0.16	4
(5Z,13E)-(15S)-9A,11A-EPIDIOXY-15-HYDROXYPROSTA-	0.13–1.61	3
GLUTATHIONE	0.6–0.75	3
PROSTAGLANDIN G1	0.05	1
PROSTAGLANDIN G2	0.16	1
PROSTAGLANDIN H1	0.01	1
PROSTAGLANDINE G2	—	0

Catalyzed reactions (Rhea), 2 shown:

• prostaglandin H2 = prostaglandin E2 (RHEA:12893)
• prostaglandin H2 = (12S)-hydroxy-(5Z,8E,10E)-heptadecatrienoate + malonaldehyde (RHEA:48644)

UniProt features (15 total): chain 2, mutagenesis site 2, topological domain 2, domain 2, binding site 2, modified residue 1, sequence variant 1, sequence conflict 1, transmembrane region 1, site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H7Z7-F1	85.07	0.71

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 87–88 (cleavage)

Ligand- & substrate-binding residues (2): 148; 164–165

Post-translational modifications (1): 95

Mutagenesis-validated functional residues (2):

Position	Phenotype
110	loss of prostaglandin-e synthase activity. can bind glutathione-heme and exhibits pgh2 degradation activity.
113	slightly decreased prostaglandin-e synthase activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-2162123	Synthesis of Prostaglandins (PG) and Thromboxanes (TX)
R-HSA-6798695	Neutrophil degranulation

MSigDB gene sets: 166 (showing top): SHEPARD_BMYB_MORPHOLINO_UP, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_THE_CH_CH_GROUP_OF_DONORS, SHEPARD_CRASH_AND_BURN_MUTANT_UP, GOBP_LONG_CHAIN_FATTY_ACID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS, PATIL_LIVER_CANCER, GOBP_SMALL_MOLECULE_BIOSYNTHETIC_PROCESS, MCBRYAN_PUBERTAL_BREAST_4_5WK_DN, MYCMAX_01, GOBP_SECRETION, GOBP_FATTY_ACID_BIOSYNTHETIC_PROCESS, GGCAGTG_MIR3243P

GO Biological Process (9): lipid metabolic process (GO:0006629), cyclooxygenase pathway (GO:0019371), positive regulation of DNA-templated transcription (GO:0045893), prostanoid biosynthetic process (GO:0046457), secretion (GO:0046903), prostaglandin biosynthetic process (GO:0001516), fatty acid metabolic process (GO:0006631), fatty acid biosynthetic process (GO:0006633), prostaglandin metabolic process (GO:0006693)

GO Molecular Function (8): DNA binding (GO:0003677), lyase activity (GO:0016829), heme binding (GO:0020037), 12-hydroxyheptadecatrienoic acid synthase activity (GO:0036134), glutathione binding (GO:0043295), prostaglandin-E synthase activity (GO:0050220), protein binding (GO:0005515), isomerase activity (GO:0016853)

GO Cellular Component (10): Golgi membrane (GO:0000139), extracellular region (GO:0005576), nucleus (GO:0005634), mitochondrion (GO:0005739), cytosol (GO:0005829), azurophil granule lumen (GO:0035578), perinuclear region of cytoplasm (GO:0048471), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Arachidonate metabolism	1
Innate Immune System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	5
cytoplasm	4
intracellular membrane-bounded organelle	3
prostanoid metabolic process	2
catalytic activity	2
primary metabolic process	1
prostaglandin biosynthetic process	1
arachidonate metabolic process	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
unsaturated fatty acid biosynthetic process	1
icosanoid biosynthetic process	1
transport	1
prostaglandin metabolic process	1
prostanoid biosynthetic process	1
lipid metabolic process	1
monocarboxylic acid metabolic process	1
fatty acid metabolic process	1
lipid biosynthetic process	1
monocarboxylic acid biosynthetic process	1
nucleic acid binding	1
tetrapyrrole binding	1
oxidoreductase activity, acting on the CH-CH group of donors, NAD or NADP as acceptor	1
anion binding	1
modified amino acid binding	1
oligopeptide binding	1
sulfur compound binding	1
intramolecular oxidoreductase activity	1
binding	1
Golgi apparatus	1
bounding membrane of organelle	1
vacuolar lumen	1
secretory granule lumen	1
azurophil granule	1
intracellular anatomical structure	1
endomembrane system	1

Protein interactions and networks

STRING

1284 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PTGES2	PTGES3	Q15185	939
PTGES2	PTGES	O14684	891
PTGES2	GLRX	P35754	824
PTGES2	TXN	P10599	708
PTGES2	PTGER1	P34995	703
PTGES2	PTGER4	P35408	672
PTGES2	PTGER3	P43115	651
PTGES2	PTGS2	P35354	648
PTGES2	C9J5N1	C9J5N1	640
PTGES2	HPGD	P15428	639
PTGES2	PTGS1	P23219	636
PTGES2	AKR1C3	P42330	613
PTGES2	TBXAS1	P24557	602
PTGES2	PTGIS	Q16647	598
PTGES2	IL6	P05231	552

IntAct

76 interactions, top by confidence:

A	B	Type	Score
PTGES2	rep	psi-mi:“MI:0915”(physical association)	0.660
UQCRQ	COX7A2L	psi-mi:“MI:0914”(association)	0.640
RANBP6	SLC27A2	psi-mi:“MI:0914”(association)	0.640
TRDN	TMEM223	psi-mi:“MI:0914”(association)	0.640
PTGES2	CFAP141	psi-mi:“MI:0915”(physical association)	0.560
CFAP141	PTGES2	psi-mi:“MI:0915”(physical association)	0.560
DLK1	TCAF2	psi-mi:“MI:0914”(association)	0.530
LRP1	NME4	psi-mi:“MI:0914”(association)	0.530
ABCF2	AHCYL1	psi-mi:“MI:0914”(association)	0.530
TMEM267	ECPAS	psi-mi:“MI:0914”(association)	0.530
SHISA2	CEP170P1	psi-mi:“MI:0914”(association)	0.530
rep	AGPS	psi-mi:“MI:0914”(association)	0.530
PBXIP1	GOLIM4	psi-mi:“MI:0914”(association)	0.530
PTGES2	HTT	psi-mi:“MI:0915”(physical association)	0.400
PTGES2	ADRB2	psi-mi:“MI:0915”(physical association)	0.370
MYC	ILVBL	psi-mi:“MI:0914”(association)	0.350
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
SCGB2A2	GXYLT2	psi-mi:“MI:0914”(association)	0.350
ATP6V0D1		psi-mi:“MI:0914”(association)	0.350
EID3	ACSL4	psi-mi:“MI:0914”(association)	0.350
FUZ	UBB	psi-mi:“MI:0914”(association)	0.350
COQ9	NDUFS8	psi-mi:“MI:0914”(association)	0.350
NDUFA4	NUDT19	psi-mi:“MI:0914”(association)	0.350

BioGRID (125): C1orf189 (Two-hybrid), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS), PTGES2 (Affinity Capture-MS)

ESM2 similar proteins: A0PJW6, A5PJW2, B3DI94, B5DFG1, O00411, O95382, P49753, Q059A4, Q0V9C9, Q3SX05, Q4KLZ1, Q4KM93, Q4R5Q4, Q4VAE3, Q53S58, Q5EA71, Q5T1A1, Q5XIC2, Q643R3, Q66LN0, Q6DC58, Q6NVG1, Q76MJ5, Q7YS91, Q80YU0, Q863F8, Q8BPE4, Q8BWM0, Q8N159, Q8NFF5, Q8VCA6, Q8VD26, Q921N7, Q96AN5, Q96KR6, Q99MQ3, Q9BQ95, Q9BUB7, Q9BYK8, Q9CQE2

Diamond homologs: Q66LN0, Q7ZUC7, Q8BWM0, Q9H7Z7, Q9N0A4

SIGNOR signaling

2 interactions.

A	Effect	B	Mechanism
PTGES2	“up-regulates quantity”	“prostaglandin E2(1-)”	“chemical modification”
PTGES2	“up-regulates quantity”	“prostaglandin H2(1-)”	“chemical modification”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 93 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Complex III assembly	5	36.0×	1e-04
Peroxisomal protein import	5	14.2×	5e-03
Respiratory electron transport	7	10.9×	9e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	49
Likely benign	3
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1779 predictions. Top by Δscore:

Variant	Effect	Δscore
9:128121270:CCGC:C	acceptor_gain	1.0000
9:128121271:CGCC:C	acceptor_gain	1.0000
9:128121274:C:CC	acceptor_gain	1.0000
9:128122358:TCAC:T	donor_loss	1.0000
9:128122359:CACCA:C	donor_loss	1.0000
9:128122360:A:AC	donor_gain	1.0000
9:128122360:ACC:A	donor_loss	1.0000
9:128122361:C:CC	donor_gain	1.0000
9:128122475:GGTGC:G	acceptor_gain	1.0000
9:128122476:GTGC:G	acceptor_gain	1.0000
9:128122477:TGC:T	acceptor_gain	1.0000
9:128122478:GC:G	acceptor_gain	1.0000
9:128122479:CC:C	acceptor_gain	1.0000
9:128122480:C:CA	acceptor_loss	1.0000
9:128122480:C:CC	acceptor_gain	1.0000
9:128122485:C:CT	acceptor_gain	1.0000
9:128122486:G:T	acceptor_gain	1.0000
9:128122927:CA:C	donor_gain	1.0000
9:128122928:A:AC	donor_gain	1.0000
9:128122929:C:CC	donor_gain	1.0000
9:128123130:CCTCC:C	acceptor_gain	1.0000
9:128123131:CTCC:C	acceptor_gain	1.0000
9:128123131:CTCCC:C	acceptor_gain	1.0000
9:128123132:TCCC:T	acceptor_loss	1.0000
9:128123132:TCCCT:T	acceptor_gain	1.0000
9:128123133:CC:C	acceptor_gain	1.0000
9:128123134:CC:C	acceptor_gain	1.0000
9:128123134:CCTGC:C	acceptor_loss	1.0000
9:128123135:C:CC	acceptor_gain	1.0000
9:128123135:CT:C	acceptor_loss	1.0000

AlphaMissense

2423 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:128125275:G:T	P149H	0.999
9:128125382:G:C	C113W	0.999
9:128125383:C:T	C113Y	0.999
9:128125385:G:C	F112L	0.999
9:128125385:G:T	F112L	0.999
9:128125387:A:G	F112L	0.999
9:128123117:C:G	R235P	0.998
9:128124518:G:C	S170R	0.998
9:128124518:G:T	S170R	0.998
9:128124520:T:G	S170R	0.998
9:128125408:A:C	Y105D	0.998
9:128122427:A:G	W314R	0.997
9:128122427:A:T	W314R	0.997
9:128123038:A:C	F261L	0.997
9:128123038:A:T	F261L	0.997
9:128123040:A:G	F261L	0.997
9:128123052:C:G	A257P	0.997
9:128123121:A:G	W234R	0.997
9:128123121:A:T	W234R	0.997
9:128125376:C:A	K115N	0.997
9:128125376:C:G	K115N	0.997
9:128125384:A:G	C113R	0.997
9:128122967:G:T	A285D	0.996
9:128123110:C:A	W237C	0.996
9:128123110:C:G	W237C	0.996
9:128123112:A:G	W237R	0.996
9:128123112:A:T	W237R	0.996
9:128125275:G:C	P149R	0.996
9:128125276:G:A	P149S	0.996
9:128125383:C:A	C113F	0.996

dbSNP variants (sampled 300 via entrez): RS1000258062 (9:128122013 C>A,T), RS1000262039 (9:128125481 C>T), RS1000421357 (9:128120655 T>C), RS1000515000 (9:128129091 C>G,T), RS1001042743 (9:128126970 G>A), RS1001076923 (9:128126671 C>G), RS1001159700 (9:128127502 C>CAGCCCCAGGGCT), RS1001269176 (9:128124139 G>A), RS1001292002 (9:128126418 G>C), RS1001411343 (9:128121318 C>A), RS1002528183 (9:128127802 C>A,T), RS1003122383 (9:128126669 G>A), RS1003447883 (9:128129065 A>C,G), RS1003523756 (9:128128214 C>G,T), RS1003696440 (9:128120607 C>A,T)

Disease associations

OMIM: gene MIM:608152 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST005951_65	Body mass index	5.000000e-09

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4411 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 16,169 (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
CHEMBL307261	ARTENIMOL	4	21
CHEMBL361497	ARTESUNATE	4	392
CHEMBL566534	ARTEMETHER	4	88
CHEMBL269671	ARTEMISININ	3	15,668

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Prostaglandin synthases

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
compound 30 [PMID: 15953724]	Inhibition	6.0	pIC50

Binding affinities (BindingDB)

239 measured of 239 human assays (239 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[[3-(5-chloro-6-methoxy-3-pyridinyl)phenyl]sulfonylamino]benzenesulfonamide	IC50	22 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[6-[2-[4-(trifluoromethyl)phenyl]ethynyl]-3-pyridinyl]ethylsulfonylamino]benzenesulfonamide	IC50	31 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(4-chloro-2-methoxyphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	36 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(1-benzofuran-2-yl)phenyl]ethenyl]sulfonylamino]-4-fluorobenzenesulfonamide	IC50	40 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(2-cyclopentylethynyl)phenyl]ethylsulfonylamino]-5-(hydroxymethyl)benzenesulfonamide	IC50	41 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(furan-2-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	44 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(3,3-dimethylbut-1-ynyl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	55 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-fluoro-6-[[(E)-2-[4-(furan-2-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	57 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(1-benzofuran-2-yl)phenyl]ethenyl]sulfonylamino]-6-fluorobenzenesulfonamide	IC50	74 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(4-bromophenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	74 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(3,3-dimethylbut-1-ynyl)phenyl]ethylsulfonylamino]-5-(hydroxymethyl)benzenesulfonamide	IC50	75 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(3,4-dichlorophenyl)ethenyl]sulfonylamino]-6-fluorobenzenesulfonamide	IC50	77 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(1-benzofuran-2-yl)phenyl]ethenyl]sulfonylamino]-5-fluorobenzenesulfonamide	IC50	79 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(3,3-dimethylbut-1-ynyl)phenyl]ethylsulfonylamino]benzenesulfonamide	IC50	81 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
5-fluoro-2-[[(E)-2-(4-phenylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	84 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-fluoro-2-[[(E)-2-naphthalen-2-ylethenyl]sulfonylamino]benzenesulfonamide	IC50	91 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(cyclopenten-1-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	97 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-[4-(trifluoromethyl)phenyl]phenyl]ethylsulfonylamino]benzenesulfonamide	IC50	100 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(difluoromethoxy)phenyl]ethenyl]sulfonylamino]-6-fluorobenzenesulfonamide	IC50	110 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[2-(difluoromethoxy)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	110 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-fluoro-2-[[(E)-2-[4-(furan-2-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	120 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(1-benzofuran-2-yl)phenyl]ethylsulfonylamino]benzenesulfonamide	IC50	130 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-fluoro-6-[[(E)-2-(4-phenylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	130 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	130 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-chloro-2-[2-(4-chloro-2-methoxyphenyl)ethylsulfonylamino]benzenesulfonamide	IC50	130 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-chloro-2-[2-(3,4-dichlorophenyl)ethylsulfonylamino]benzenesulfonamide	IC50	130 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(1-benzofuran-2-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	140 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-(4-bromophenyl)ethylsulfonylamino]benzenesulfonamide	IC50	140 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
5-chloro-2-[2-(3,4-dichlorophenyl)ethylsulfonylamino]-4-fluorobenzenesulfonamide	IC50	150 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-fluoro-2-[[(E)-2-(4-methylsulfanylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	160 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
4-fluoro-2-[[(E)-2-(4-phenylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	160 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
5-fluoro-2-[[(E)-2-[4-(furan-2-yl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	170 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-[4-(trifluoromethyl)phenyl]phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	180 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(furan-2-yl)phenyl]ethylsulfonylamino]benzenesulfonamide	IC50	190 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-naphthalen-2-ylethenyl]sulfonylamino]benzenesulfonamide	IC50	190 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[3-(5-fluoro-6-methoxy-3-pyridinyl)phenyl]sulfonylamino]benzenesulfonamide	IC50	190 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
5-fluoro-2-[[(E)-2-(4-methylsulfanylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	220 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-(4-tert-butylphenyl)ethylsulfonylamino]benzenesulfonamide	IC50	220 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[3-[3-(trifluoromethoxy)phenyl]phenyl]sulfonylamino]benzenesulfonamide	IC50	220 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[3-(3,4-dichlorophenyl)phenyl]sulfonylamino]benzenesulfonamide	IC50	220 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-[4-(3-hydroxy-3-methylbut-1-ynyl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	220 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-(4-chloro-2-methoxyphenyl)ethylsulfonylamino]benzenesulfonamide	IC50	250 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[4-(2,3-dihydro-1-benzofuran-2-yl)phenyl]ethylsulfonylamino]benzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(3,4-dichlorophenyl)ethenyl]sulfonylamino]-4-fluorobenzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(5-bromo-2-methoxyphenyl)ethenyl]sulfonylamino]-5-fluorobenzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
5-fluoro-2-[[(E)-2-[3-(trifluoromethyl)phenyl]ethenyl]sulfonylamino]benzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-(4-cyclopentylphenyl)ethylsulfonylamino]benzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[2-[6-(2-cyclohexylethynyl)-3-pyridinyl]ethylsulfonylamino]benzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[[(E)-2-(2-methylsulfanylphenyl)ethenyl]sulfonylamino]benzenesulfonamide	IC50	270 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy
2-[1-(4-chlorophenyl)propan-2-ylsulfonylamino]benzenesulfonamide	IC50	280 nM	US-9145380: Bis-(sulfonylamino) derivatives for use in therapy

ChEMBL bioactivities

279 potent at pChembl≥5 of 285 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.52	IC50	3	nM	CHEMBL180650
8.40	IC50	4	nM	CHEMBL180617
8.30	IC50	5	nM	CHEMBL369525
8.22	IC50	6	nM	CHEMBL368241
8.15	IC50	7	nM	CHEMBL182032
8.10	IC50	8	nM	CHEMBL362836
7.92	IC50	12	nM	CHEMBL181728
7.80	IC50	16	nM	CHEMBL362242
7.66	IC50	22	nM	CHEMBL362675
7.66	IC50	22	nM	CHEMBL3962955
7.51	IC50	31	nM	CHEMBL183596
7.51	IC50	31	nM	CHEMBL3986331
7.50	IC50	32	nM	CHEMBL181792
7.48	IC50	33	nM	CHEMBL183878
7.44	IC50	36	nM	CHEMBL3904203
7.40	IC50	40	nM	CHEMBL3897379
7.39	IC50	41	nM	CHEMBL3961959
7.36	IC50	44	nM	CHEMBL3943504
7.26	IC50	55	nM	CHEMBL3943346
7.24	IC50	57	nM	CHEMBL3965498
7.13	IC50	74	nM	CHEMBL3968523
7.13	IC50	74	nM	CHEMBL3966442
7.12	IC50	75	nM	CHEMBL3930981
7.11	IC50	77	nM	CHEMBL3942994
7.10	IC50	79	nM	CHEMBL3898952
7.09	IC50	81	nM	CHEMBL3935976
7.08	IC50	84	nM	CHEMBL3951095
7.04	IC50	91	nM	CHEMBL3957120
7.01	IC50	97	nM	CHEMBL3918947
7.00	IC50	100	nM	CHEMBL3946465
6.96	IC50	110	nM	CHEMBL3908925
6.96	IC50	110	nM	CHEMBL3941676
6.92	IC50	120	nM	CHEMBL3889985
6.89	IC50	130	nM	CHEMBL3959989
6.89	IC50	130	nM	CHEMBL3907650
6.89	IC50	130	nM	CHEMBL3975393
6.89	IC50	130	nM	CHEMBL3903992
6.89	IC50	130	nM	CHEMBL3951825
6.85	IC50	140	nM	CHEMBL3906349
6.85	IC50	140	nM	CHEMBL3943912
6.82	IC50	150	nM	CHEMBL3911159
6.80	IC50	160	nM	CHEMBL180846
6.80	IC50	160	nM	CHEMBL3960265
6.80	IC50	160	nM	CHEMBL3891144
6.77	IC50	170	nM	CHEMBL3960306
6.75	IC50	180	nM	CHEMBL3913683
6.72	IC50	190	nM	CHEMBL3968505
6.72	IC50	190	nM	CHEMBL3928194
6.72	IC50	190	nM	CHEMBL3923779
6.66	IC50	220	nM	CHEMBL3977611

PubChem BioAssay actives

39 with measured affinity, of 159 total; 35 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-[1-[(4-chlorophenyl)methyl]-5-[3-fluoro-4-(2-methylphenyl)phenyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0030	uM
3-[5-[4-(2-chlorophenyl)-3-fluorophenyl]-1-[(4-chlorophenyl)methyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0040	uM
3-[1-[(4-chlorophenyl)methyl]-5-[3-fluoro-4-(2-methoxyphenyl)phenyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0050	uM
3-[5-[4-(2-acetylphenyl)-3-fluorophenyl]-1-[(4-chlorophenyl)methyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0060	uM
3-[1-[(4-chlorophenyl)methyl]-5-(3-fluoro-4-phenylphenyl)-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0070	uM
3-[1-[(4-chlorophenyl)methyl]-5-[3-fluoro-4-(2-fluorophenyl)phenyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0080	uM
3-[1-[(4-chlorophenyl)methyl]-5-(3-fluoro-4-pyridin-3-ylphenyl)-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0120	uM
3-[1-[(4-chlorophenyl)methyl]-3-methyl-5-(4-phenylphenyl)indol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0160	uM
3-[1-[(4-chlorophenyl)methyl]-5-(3-chloro-4-phenylphenyl)-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0220	uM
3-[1-[(4-chlorophenyl)methyl]-5-[3-fluoro-4-(4-methylphenyl)phenyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0310	uM
3-[1-[(4-chlorophenyl)methyl]-5-(3-fluoro-4-pyrazin-2-ylphenyl)-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0320	uM
3-[1-[(4-chlorophenyl)methyl]-5-[3-fluoro-4-(3-methylphenyl)phenyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.0330	uM
3-[1-[(4-chlorophenyl)methyl]-3-methyl-5-(3-phenylphenyl)indol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.1600	uM
3-[1-[(4-chlorophenyl)methyl]-3-(3,3-dimethylbutanoyl)-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.2500	uM
3-[3-(2-tert-butylsulfanylacetyl)-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.2600	uM
3-[3-[(4-tert-butylphenyl)methyl]-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.2900	uM
3-[5-tert-butyl-1-[(4-chlorophenyl)methyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.3300	uM
(1R,4S,5R,8S,9R,12S,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-one	2099796: Binding affinity to human mPGES-2 (1 to 87 residues) assessed as dissociation constant	kd	0.5300	uM
3-[1-[(4-chlorophenyl)methyl]-3-methyl-5-phenylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.6000	uM
3-[1-[(4-chlorophenyl)methyl]-3-phenoxy-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.6500	uM
3-[1-[(4-chlorophenyl)methyl]-3-(2-methylbenzoyl)-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	0.9000	uM
3-[1-[(4-chlorophenyl)methyl]-3-methyl-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	1.1000	uM
3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	1.6000	uM
4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid	2099754: Displacement of ART-P1 from heme-free recombinant mPGES-2 (unknown origin) assessed as inhibition of ART-P1 binding to mPGES-2 incubated for 1 hr followed by ART-P1 addition for 30 mins by competitive labeling gel fluorescence assay	ic50	1.6000	uM
3-[1-[(4-chlorophenyl)methyl]-5-fluoro-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	2.6000	uM
3-[1-[(4-chlorophenyl)methyl]-3-methylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	3.2000	uM
3-[3-tert-butylsulfanyl-1-(3-phenylpropyl)-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	3.2000	uM
3-nitro-4-[[4-(4-phenylphenyl)triazol-1-yl]methyl]benzoic acid	588175: Inhibition of Prostaglandin E2 synthase-1 in IL1-beta stimulated microsomal fraction of human A549 cell assessed as PGE2 level by RP-HPLC	ic50	3.2000	uM
3-[1-[(4-chlorophenyl)methyl]-3-methyl-7-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	4.3000	uM
[(1S,4S,5R,8S,9R,10R,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl] benzoate	2099754: Displacement of ART-P1 from heme-free recombinant mPGES-2 (unknown origin) assessed as inhibition of ART-P1 binding to mPGES-2 incubated for 1 hr followed by ART-P1 addition for 30 mins by competitive labeling gel fluorescence assay	ic50	5.9000	uM
3-[1-[(4-chlorophenyl)methyl]-3-phenyl-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	6.4000	uM
3-(3-tert-butylsulfanyl-5-propan-2-yl-1-prop-2-enylindol-2-yl)-2,2-dimethylpropanoic acid	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	6.7000	uM
methyl 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoate	240920: Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	ic50	7.2000	uM
(1R,4S,5R,8S,9R,10S,12R,13R)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecane	2099754: Displacement of ART-P1 from heme-free recombinant mPGES-2 (unknown origin) assessed as inhibition of ART-P1 binding to mPGES-2 incubated for 1 hr followed by ART-P1 addition for 30 mins by competitive labeling gel fluorescence assay	ic50	7.2000	uM
(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-ol	2099754: Displacement of ART-P1 from heme-free recombinant mPGES-2 (unknown origin) assessed as inhibition of ART-P1 binding to mPGES-2 incubated for 1 hr followed by ART-P1 addition for 30 mins by competitive labeling gel fluorescence assay	ic50	9.6000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	3
bisphenol A	decreases expression	2
Arsenic	increases expression, affects methylation, affects cotreatment, decreases expression, increases abundance	2
Benzo(a)pyrene	decreases methylation, increases expression	2
Lipopolysaccharides	increases expression, decreases reaction, increases activity, increases chemical synthesis, affects cotreatment	2
bisphenol F	increases expression	1
2,4,6-tribromophenol	decreases expression	1
pirinixic acid	decreases activity	1
diethyl phthalate	affects reaction, decreases expression, affects cotreatment	1
decabromobiphenyl ether	decreases expression	1
diisononyl phthalate	affects cotreatment, affects reaction, decreases expression	1
beta-lapachone	increases expression	1
tetrabromobisphenol A	decreases expression	1
perfluorooctanoic acid	increases expression	1
diisobutyl phthalate	affects cotreatment, affects reaction, decreases expression	1
butylbenzyl phthalate	affects cotreatment, affects reaction, decreases expression	1
2-chloroethyl ethyl sulfide	increases expression	1
pinosylvin	decreases expression	1
di-n-butylphosphoric acid	affects expression	1
2-palmitoylglycerol	increases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid	affects binding, decreases activity, decreases reaction, increases activity, increases chemical synthesis	1
bisphenol AF	increases expression	1
Resveratrol	affects cotreatment, decreases reaction, increases expression	1
Air Pollutants	increases abundance, increases expression	1
Diacetyl	increases expression	1
Dibutyl Phthalate	affects reaction, decreases expression, affects cotreatment	1
Diethylhexyl Phthalate	affects cotreatment, affects reaction, decreases expression	1
Diethylstilbestrol	decreases expression	1

ChEMBL screening assays

50 unique, capped per target: 50 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1050561	Binding	Inhibition of human PGES2	Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. — Bioorg Med Chem Lett

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B7YZ	Abcam Raji PTGES2 KO	Cancer cell line	Male
CVCL_B9ZQ	Abcam THP-1 PTGES2 KO	Cancer cell line	Male
CVCL_C7BE	Abcam PC-3 PTGES2 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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