OXER1

gene
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Also known as GPCRTG1019GPR170

Summary

OXER1 (oxoeicosanoid receptor 1, HGNC:24884) is a protein-coding gene on chromosome 2p21, encoding Oxoeicosanoid receptor 1 (Q8TDS5). Receptor for eicosanoids and polyunsaturated fatty acids such as 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-OXO-ETE), 5(S)-hydroperoxy-6E,8Z,11Z,14Z-eicosatetraenoic acid (5(S)-HPETE) and arachidonic acid.

Enables G protein-coupled receptor activity and icosanoid binding activity. Involved in adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 165140 — RefSeq curated summary.

At a glance

  • GWAS associations: 3
  • Clinical variants (ClinVar): 109 total — 1 pathogenic
  • Druggable target: yes — 3 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_148962

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:24884
Approved symbolOXER1
Nameoxoeicosanoid receptor 1
Location2p21
Locus typegene with protein product
StatusApproved
AliasesGPCR, TG1019, GPR170
Ensembl geneENSG00000162881
Ensembl biotypeprotein_coding
OMIM620064
Entrez165140

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000378661

RefSeq mRNA: 1 — MANE Select: NM_148962 NM_148962

CCDS: CCDS1810

Canonical transcript exons

ENST00000378661 — 1 exons

ExonStartEnd
ENSE000014782764276249942764135

Expression profiles

Bgee: expression breadth ubiquitous, 155 present calls, max score 90.79.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.7244 / max 137.4396, expressed in 147 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
280230.5619122
280210.107251
280220.055323

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
right lobe of liverUBERON:000111490.79gold quality
mucosa of transverse colonUBERON:000499184.89gold quality
liverUBERON:000210778.93gold quality
bloodUBERON:000017878.39gold quality
right ovaryUBERON:000211877.05gold quality
granulocyteCL:000009476.87gold quality
left ovaryUBERON:000211976.65gold quality
small intestine Peyer’s patchUBERON:000345476.15gold quality
leukocyteCL:000073875.40gold quality
monocyteCL:000057675.20gold quality
small intestineUBERON:000210874.27gold quality
body of pancreasUBERON:000115073.81gold quality
ascending aortaUBERON:000149671.97gold quality
thoracic aortaUBERON:000151571.70gold quality
ovaryUBERON:000099271.62gold quality
metanephros cortexUBERON:001053371.45gold quality
adult mammalian kidneyUBERON:000008271.25gold quality
descending thoracic aortaUBERON:000234571.14gold quality
bone marrow cellCL:000209270.56gold quality
endocervixUBERON:000045870.21gold quality
mucosa of stomachUBERON:000119970.15gold quality
ectocervixUBERON:001224969.91gold quality
transverse colonUBERON:000115769.71gold quality
body of uterusUBERON:000985369.71gold quality
cortex of kidneyUBERON:000122569.64gold quality
spleenUBERON:000210669.37gold quality
right coronary arteryUBERON:000162568.96gold quality
bone marrowUBERON:000237168.67gold quality
sural nerveUBERON:001548868.58gold quality
aortaUBERON:000094768.43gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no0.89

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

9 targeting OXER1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-320299.6667.702737
HSA-MIR-6727-3P99.4965.921333
HSA-MIR-4722-3P99.3565.221099
HSA-MIR-6780B-3P99.1367.18622
HSA-MIR-950098.6266.541845
HSA-MIR-6801-3P98.0464.64805
HSA-MIR-430398.0168.132304
HSA-MIR-6810-3P97.9664.571023
HSA-MIR-369096.4465.18737

Literature-anchored findings (GeneRIF, showing 11)

  • Identification of a novel human receptor coupled to G(i/o). (PMID:12065583)
  • identification and cloning of a novel GPCR, R527; 5-oxo-ETE was identified as the ligand for R527; very high level of mRNA expression in eosinophils with high expression also detected in neutrophils and lung macrophages (PMID:12606753)
  • 5-oxoER is critical for prostate cancer cell survival. (PMID:16289380)
  • OXER1 has a role in regulating the survival-promoting effects of arachidonate 5-lipoxygenase in prostate cancer cells (PMID:23643940)
  • Gue1654 as a non-Galphai-biased antagonist of OXE-R that provides a new basis for therapeutic intervention in inflammatory diseases that involve activation of eosinophils, neutrophils, and monocytes. (PMID:24733850)
  • membrane receptor OxeR1 is involved in StAR protein induction and activation of steroidogenesis triggered by cAMP or angiotensin II, acting, at least in part, through ERK1/2 activation. (PMID:25657046)
  • These findings verify that membrane-acting androgens exert specific effects through an antagonistic interaction with OXER1. Additionally, this interaction between androgen and OXER1, which is an arachidonic acid metabolite receptor expressed in prostate cancer, provides a novel link between steroid and lipid actions and renders OXER1 as new player in the disease. (PMID:28290516)
  • The G protein coupled oxo-eicosanoid receptor 1 (OXER1) (a receptor of the arachidonic acid metabolite, 5-oxoeicosatetraenoic acid, 5-oxoETE) is as a novel mAR involved in the rapid effects of androgens. (PMID:30707908)
  • OXER1 mediates testosterone-induced calcium responses in prostate cancer cells. (PMID:34634385)
  • Enhanced OXER1 expression is indispensable for human cancer cell migration. (PMID:34775286)
  • Biological Roles of 5-Oxo-6,8,11,14-Eicosatetraenoic Acid and the OXE Receptor in Allergic Diseases: Collegium Internationale Allergologicum Update 2024. (PMID:38176394)

Cross-species orthologs

2 orthologs

OrganismSymbolGene ID
danio_reriohcar1-3ENSDARG00000062874
danio_reriohcar1-4ENSDARG00000087084

Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR2 (ENSG00000126262), FFAR1 (ENSG00000126266), OXGR1 (ENSG00000165621), P2RY1 (ENSG00000169860), P2RY6 (ENSG00000171631), GPR82 (ENSG00000171657), P2RY2 (ENSG00000175591), HCAR2 (ENSG00000182782), FFAR3 (ENSG00000185897), P2RY4 (ENSG00000186912), HCAR1 (ENSG00000196917), SUCNR1 (ENSG00000198829), HCAR3 (ENSG00000255398)

Protein

Protein identifiers

Oxoeicosanoid receptor 1Q8TDS5 (reviewed: Q8TDS5)

Alternative names: 5-oxo-ETE G-protein coupled receptor, G-protein coupled receptor 170, G-protein coupled receptor R527, G-protein coupled receptor TG1019

All UniProt accessions (1): Q8TDS5

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for eicosanoids and polyunsaturated fatty acids such as 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-OXO-ETE), 5(S)-hydroperoxy-6E,8Z,11Z,14Z-eicosatetraenoic acid (5(S)-HPETE) and arachidonic acid. Seems to be coupled to the G(i)/G(o), families of heteromeric G proteins.

Subcellular location. Membrane.

Tissue specificity. Expressed in various tissues except brain. Expression is more intense in liver, kidney, peripheral leukocyte, lung, and spleen than in other tissues. Highly expressed in eosinophils, neutrophils, and lung macrophages.

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

RefSeq proteins (1): NP_683765* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR017452GPCR_Rhodpsn_7TMDomain
IPR051893HCARsFamily

Pfam: PF00001

UniProt features (22 total): topological domain 8, transmembrane region 7, sequence variant 2, chain 1, region of interest 1, compositionally biased region 1, glycosylation site 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q8TDS5-F182.240.47

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): 126–198

Glycosylation sites (1): 5

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-391903Eicosanoid ligand-binding receptors
R-HSA-418594G alpha (i) signalling events

MSigDB gene sets: 32 (showing top): REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_ADENYLATE_CYCLASE_INHIBITING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOMF_LONG_CHAIN_FATTY_ACID_BINDING, GOMF_FATTY_ACID_BINDING, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_ORGANIC_ACID_BINDING, GOMF_LIPID_BINDING, GOMF_MONOCARBOXYLIC_ACID_BINDING, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, KRIGE_RESPONSE_TO_TOSEDOSTAT_6HR_DN, MARTENS_TRETINOIN_RESPONSE_UP, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOMF_ICOSANOID_BINDING

GO Biological Process (3): G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), signal transduction (GO:0007165)

GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), 5-oxo-6E,8Z,11Z,14Z-icosatetraenoic acid binding (GO:0050646), 5-hydroxy-6E,8Z,11Z,14Z-icosatetraenoic acid binding (GO:0050647), 5(S)-hydroxyperoxy-6E,8Z,11Z,14Z-icosatetraenoic acid binding (GO:0050648), protein binding (GO:0005515)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Class A/1 (Rhodopsin-like receptors)1
GPCR downstream signalling1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
long-chain fatty acid binding3
icosanoid binding3
fatty acid derivative binding2
G protein-coupled receptor activity1
signal transduction1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway1
adenylate cyclase inhibitor activity1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
transmembrane signaling receptor activity1
G protein-coupled receptor signaling pathway1
binding1
membrane1
cell periphery1
cellular anatomical structure1

Protein interactions and networks

STRING

508 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
OXER1GPRC6AQ5T6X5622
OXER1SLC39A9Q9NUM3621
OXER1LTB4R2Q9NPC1513
OXER1ALOX5P09917507
OXER1TRPM8Q7Z2W7398
OXER1GPR148Q8TDV2380
OXER1ALOX5APP20292348
OXER1OR4D1Q15615320
OXER1NPBQ8NG41312
OXER1OR2A14Q96R47312
OXER1TAS2R4Q9NYW5300
OXER1ZNF786Q8N393297
OXER1ALOX12P18054270
OXER1ZNF30P17039268
OXER1MRGPRDQ8TDS7267
OXER1TRHRP34981267

IntAct

135 interactions, top by confidence:

ABTypeScore
LASP1OXER1psi-mi:“MI:0915”(physical association)0.560
RECKOXER1psi-mi:“MI:0915”(physical association)0.560
OXER1ASB13psi-mi:“MI:0915”(physical association)0.560
OXER1TFGpsi-mi:“MI:0915”(physical association)0.560
PRR20DOXER1psi-mi:“MI:0915”(physical association)0.560
EFCAB3OXER1psi-mi:“MI:0915”(physical association)0.560
KRTAP19-5OXER1psi-mi:“MI:0915”(physical association)0.560
CRYBA2OXER1psi-mi:“MI:0915”(physical association)0.560
TP53BP1OXER1psi-mi:“MI:0915”(physical association)0.560
TLE5OXER1psi-mi:“MI:0915”(physical association)0.560
OXER1PLSCR4psi-mi:“MI:0915”(physical association)0.560
OXER1ANAPC11psi-mi:“MI:0915”(physical association)0.560
OXER1RNF38psi-mi:“MI:0915”(physical association)0.560
JMJD7OXER1psi-mi:“MI:0915”(physical association)0.560
ZIC1OXER1psi-mi:“MI:0915”(physical association)0.560
OXER1ZC3H10psi-mi:“MI:0915”(physical association)0.560
HNF1BOXER1psi-mi:“MI:0915”(physical association)0.560
OTX1OXER1psi-mi:“MI:0915”(physical association)0.560
CCNKOXER1psi-mi:“MI:0915”(physical association)0.560
FOXH1OXER1psi-mi:“MI:0915”(physical association)0.560
RNF44OXER1psi-mi:“MI:0915”(physical association)0.560
VGLL3OXER1psi-mi:“MI:0915”(physical association)0.560
HNRNPH1OXER1psi-mi:“MI:0915”(physical association)0.560
OXER1KRTAP4-2psi-mi:“MI:0915”(physical association)0.560
PRKAB2OXER1psi-mi:“MI:0915”(physical association)0.560
PROP1OXER1psi-mi:“MI:0915”(physical association)0.560
OXER1RAMACpsi-mi:“MI:0915”(physical association)0.560
ESRP1OXER1psi-mi:“MI:0915”(physical association)0.560
INTS11OXER1psi-mi:“MI:0915”(physical association)0.560
KRTAP12-3OXER1psi-mi:“MI:0915”(physical association)0.560

BioGRID (50): ARRB2 (FRET), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid), OXER1 (Two-hybrid)

ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91

Diamond homologs: A0A6I8PUB9, E9QJ73, F8VQN3, O00270, O09047, O42179, O55197, P21109, P25024, P25025, P35344, P35383, P41231, P41232, P46092, P49019, P55920, P97266, Q15722, Q16581, Q28003, Q28422, Q28519, Q28807, Q2KI97, Q2YEG0, Q5REI5, Q5YA25, Q6TAC8, Q80Z39, Q8C131, Q8CIM5, Q8SQ54, Q8TDS4, Q8TDS5, Q96G91, Q99PE3, Q9BXC0, Q9EP66, Q9JL21

SIGNOR signaling

3 interactions.

AEffectBMechanism
“diisononyl phthalate”“up-regulates activity”OXER1“chemical activation”
“mono(2-ethylhexyl) phthalate”“up-regulates activity”OXER1“chemical activation”
“monoisononyl phthalate”“up-regulates activity”OXER1“chemical activation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 46 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:

PathwayPartnersFoldFDR
Keratinization59.3×9e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic1
Likely pathogenic0
Uncertain significance97
Likely benign9
Benign2

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
59144GRCh38/hg38 2p21(chr2:41999414-42915744)x3Pathogenic

SpliceAI

69 predictions. Top by Δscore:

VariantEffectΔscore
2:42763597:C:CTdonor_gain0.8300
2:42763598:C:CTdonor_gain0.8200
2:42763593:TGCAC:Tdonor_gain0.6800
2:42763596:A:ACdonor_gain0.6300
2:42763599:A:AAdonor_gain0.4800
2:42763462:AGCTG:Aacceptor_gain0.4700
2:42764104:TTC:Tdonor_gain0.4600
2:42764105:TCT:Tdonor_gain0.4600
2:42763268:G:GTacceptor_gain0.4500
2:42763269:T:TTacceptor_gain0.4500
2:42763595:CA:Cdonor_gain0.4500
2:42763579:G:Cdonor_gain0.4000
2:42763543:C:CTdonor_gain0.3400
2:42763463:GCT:Gacceptor_gain0.3300
2:42763818:G:GCacceptor_gain0.3300
2:42763572:CGG:Cdonor_gain0.3200
2:42763362:A:ACdonor_gain0.3100
2:42763363:C:CCdonor_gain0.3100
2:42763583:G:Cdonor_gain0.3100
2:42763594:GCACC:Gdonor_gain0.3100
2:42763815:CGCG:Cacceptor_gain0.3100
2:42763818:G:Cacceptor_gain0.3100
2:42763911:A:Tacceptor_gain0.3000
2:42762661:G:Adonor_gain0.2900
2:42763279:C:CTdonor_gain0.2900
2:42763267:TG:Tacceptor_gain0.2800
2:42763814:CCGCG:Cacceptor_gain0.2800
2:42763317:G:Adonor_gain0.2700
2:42763456:C:CAacceptor_gain0.2600
2:42763544:C:CTdonor_gain0.2600

AlphaMissense

2705 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
2:42763256:G:CF308L0.982
2:42763256:G:TF308L0.982
2:42763258:A:GF308L0.982
2:42763247:G:CS311R0.979
2:42763247:G:TS311R0.979
2:42763249:T:GS311R0.979
2:42763781:G:CS133R0.977
2:42763781:G:TS133R0.977
2:42763783:T:GS133R0.977
2:42763136:A:CS348R0.975
2:42763136:A:TS348R0.975
2:42763138:T:GS348R0.975
2:42763706:C:AW158C0.973
2:42763706:C:GW158C0.973
2:42763766:G:CD138E0.970
2:42763766:G:TD138E0.970
2:42763397:G:CF261L0.960
2:42763397:G:TF261L0.960
2:42763399:A:GF261L0.960
2:42763169:G:CF337L0.959
2:42763169:G:TF337L0.959
2:42763171:A:GF337L0.959
2:42763643:G:CS179R0.954
2:42763643:G:TS179R0.954
2:42763645:T:GS179R0.954
2:42763127:G:CD351E0.947
2:42763127:G:TD351E0.947
2:42763847:A:CS111R0.945
2:42763847:A:TS111R0.945
2:42763849:T:GS111R0.945

dbSNP variants (sampled 300 via entrez): RS1000825883 (2:42765088 C>G), RS1001198392 (2:42762293 G>A), RS1001260527 (2:42762794 G>A), RS1001605615 (2:42762986 A>G), RS1001793778 (2:42762535 A>G), RS1005124017 (2:42764692 G>C), RS1005239951 (2:42762319 C>T), RS1006024291 (2:42764438 C>G), RS1006752576 (2:42765993 A>G), RS1006913389 (2:42763212 C>T), RS1007441979 (2:42765081 C>T), RS1007577480 (2:42764820 A>G), RS1007944333 (2:42762923 G>A,C), RS1008003253 (2:42762521 T>C), RS1008580311 (2:42765862 T>C)

Disease associations

OMIM: gene MIM:620064 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

StudyTraitp-value
GCST000278_1Hyperactive-impulsive symptoms2.000000e-06
GCST000281_1Attention deficit hyperactivity disorder6.000000e-06
GCST002715_2Breastfeeding duration1.000000e-06

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0006864breastfeeding duration

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1628461 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 126,019 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL367149DOCONEXENT363,817
CHEMBL460026ICOSAPENT360,180
CHEMBL465183DIHOMO-GAMMA-LINOLENIC ACID22,022

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Leukotriene receptors

Most potent curated ligand interactions (12 total), top 12:

LigandActionAffinityParameter
S‐Y048Antagonist10.7pIC50
5-oxo-ETEFull agonist8.5pEC50
[3H]5-oxo-ETEAgonist8.4pKd
5-oxo-C20:3Full agonist8.0pEC50
5-oxo-ODEFull agonist8.0pEC50
5-oxo-15-HETEFull agonist7.7pEC50
5S-HETEFull agonist7.2pEC50
5S-HPETEFull agonist7.0pEC50
5-oxo-20-HETEFull agonist6.5pEC50
5-(6-chloro-2-hexyl-1H-indol-1-yl)-5-oxo-valeric acidAntagonist6.4pIC50
5-oxo-12-HETEAntagonist6.3pIC50
Gue1654Negative6.0pIC50

Binding affinities (BindingDB)

2 measured of 3 human assays (3 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
(Z,Z,Z)-8,11,14-Eicosatrienoic acidKI3700 nM
5,8,11,14,17-EICOSAPENTAENOIC ACIDKI6000 nM

ChEMBL bioactivities

84 potent at pChembl≥5 of 91 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.92IC500.12nMCHEMBL4283608
9.55IC500.28nMCHEMBL4287941
9.42IC500.38nMCHEMBL4281149
8.68IC502.1nMCHEMBL4282356
8.66IC502.2nMCHEMBL3341973
8.57IC502.7nMCHEMBL3341971
8.52IC503nM5-OXO-ETE
8.22IC506nMCHEMBL3115775
8.22IC506nMCHEMBL3341972
8.15IC507nMCHEMBL3115774
8.15EC507nM5-OXO-ETE
8.12IC507.5nMCHEMBL1760545
7.96IC5011nMCHEMBL4284672
7.92IC5012nMCHEMBL4277299
7.80IC5016nMCHEMBL3115775
7.77IC5017nMCHEMBL3115775
7.77IC5017nMCHEMBL3115774
7.75IC5018nMCHEMBL3115774
7.75IC5018nMCHEMBL4291346
7.64IC5023nMCHEMBL4084871
7.64IC5023nMCHEMBL4291464
7.58IC5026nMCHEMBL3115793
7.55IC5028nMCHEMBL3115775
7.55IC5028nMCHEMBL3115774
7.52IC5030nMCHEMBL3115774
7.52IC5030nMCHEMBL3115786
7.48IC5033nMCHEMBL3115775
7.42IC5038nMCHEMBL4278772
7.42IC5038nMCHEMBL4279605
7.25EC5056nMCHEMBL1682258
7.17EC5067nM5-OXO-ETE
7.09IC5081nMCHEMBL3115792
7.05IC5090nMCHEMBL3115782
6.92IC50120nMCHEMBL4277207
6.87IC50136nMCHEMBL3115783
6.85IC50141nMCHEMBL3115785
6.68IC50210nMCHEMBL4280693
6.66EC50220nM5-OXO-ETE
6.65IC50223nMCHEMBL4287509
6.58IC50260nMCHEMBL4285167
6.50IC50314nMCHEMBL3115791
6.49IC50323nMCHEMBL3115787
6.42EC50380nMCHEMBL4127146
6.40IC50400nMCHEMBL2332562
6.40IC50402nMCHEMBL3115774
6.34IC50454nMCHEMBL3115775
6.34IC50460nMCHEMBL3311230
6.30IC50500nMCHEMBL3115778
6.30IC50500nMCHEMBL1526258
6.26IC50550nMCHEMBL3115800

PubChem BioAssay actives

84 with measured affinity, of 149 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
(3S)-5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0001uM
5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0003uM
(3S)-5-[5-chloro-2-[(1S)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0004uM
5-[6-chloro-2-(5-phenylpentyl)indol-1-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0021uM
(3S)-5-(6-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assayic500.0022uM
(3R)-5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assayic500.0027uM
(6E,8Z,11Z,14Z)-5-oxoicosa-6,8,11,14-tetraenoic acid590219: Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilizationic500.0030uM
(3S)-5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assayic500.0060uM
5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0060uM
5-(6-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0070uM
(6E,8Z,11Z,14Z)-20,20,20-trifluoro-5-oxoicosa-6,8,11,14-tetraenoic acid590219: Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilizationic500.0075uM
5-[5-chloro-1-methyl-2-(5-phenylpentyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0110uM
5-[6-chloro-2-(6-phenylhexyl)indol-1-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0120uM
5-[6-chloro-2-(4-phenylbutyl)indol-1-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0180uM
(3R)-5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0230uM
5-(5-chloro-1-methyl-2-undecylindol-3-yl)-3-methyl-5-oxopentanoic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0230uM
5-(5-bromo-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0260uM
5-(6-bromo-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0300uM
5-[5-chloro-1-methyl-2-(4-phenylbutyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0380uM
5-[5-chloro-1-methyl-2-(6,6,6-trifluorohexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.0380uM
(6E,8Z,11Z,13E,15S)-15-hydroxy-5-oxoicosa-6,8,11,13-tetraenoic acid579486: Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilizationec500.0560uM
5-(6-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0810uM
5-(2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.0900uM
(3R)-5-[5-chloro-2-[(1S)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.1200uM
5-(2-hexyl-3-methylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.1360uM
5-(5-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.1410uM
5-[6-chloro-2-(3-phenylpropyl)indol-1-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.2100uM
5-[5-chloro-1-methyl-2-(3-phenylpropyl)indol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.2230uM
(3S)-5-[5-chloro-2-[(1R)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.2600uM
5-(2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.3140uM
5-(2-hexyl-6-methoxyindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.3230uM
(6E,8Z,11Z,14Z,17Z)-5-oxoicosa-6,8,11,14,17-pentaenoic acid1497846: Agonist activity at human PK-tagged OXER1 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation assayec500.3800uM
5-(6-chloroindol-1-yl)-5-oxopentanoic acid736229: Antagonist activity at OXE receptor in human neutrophils assessed as 5-oxo-ETE-induced Ca2+ mobilization incubated for 2 mins prior to 5-oxo-ETE addition measured after 1 min by spectrofluorimetric analysisic500.4000uM
5-[6-chloro-2-[(Z)-hex-1-enyl]indol-1-yl]-3-methyl-5-oxopentanoic acid1180185: Antagonist activity at 5-oxo-ETE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced Ca2+ mobilization incubated for 2 mins prior to 5-oxo-ETE addition by indo-1 staining-based spectrofluorometryic500.4600uM
(6E,8Z,10E,12S,14Z)-12-hydroxy-5-oxoicosa-6,8,10,14-tetraenoic acid1067794: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization by spectrofluorometric analysisic500.5000uM
(5Z,8Z,10E,12S,14Z)-12-hydroxyicosa-5,8,10,14-tetraenoic acid1410868: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition by fluorescence assayic500.5000uM
5-oxo-5-[2-[(Z)-undec-1-enyl]indol-1-yl]pentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.5500uM
5-(5-chloro-2-hexyl-1-methylindol-3-yl)-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.5660uM
5-(2-octylindol-1-yl)-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.5700uM
2-[1-[2-(5-chloro-2-hexyl-1-methylindol-3-yl)-2-oxoethyl]cyclopropyl]acetic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.5800uM
5-(5-bromo-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.6380uM
5-oxo-5-(2-undecylindol-1-yl)pentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.7000uM
2-[1-[2-(5-chloro-2-hexyl-1-methylindol-3-yl)-2-oxoethyl]cyclobutyl]acetic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.7200uM
(3R)-5-[5-chloro-2-[(1R)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid1410867: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic500.7500uM
5-(2-heptylindol-1-yl)-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic500.7500uM
3-(5-chloro-2-hexyl-1-methylindole-3-carbonyl)benzoic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic501.1200uM
5-(2-hexylindol-1-yl)-5-oxopentanoic acid1067795: Antagonist activity at OXE receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins prior to 5-oxo-ETE induction by spectrofluorometric analysisic501.1300uM
5-(5-chloroindol-1-yl)-5-oxopentanoic acid736229: Antagonist activity at OXE receptor in human neutrophils assessed as 5-oxo-ETE-induced Ca2+ mobilization incubated for 2 mins prior to 5-oxo-ETE addition measured after 1 min by spectrofluorimetric analysisic501.1700uM
5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3,3-dimethyl-5-oxopentanoic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic501.3300uM
4-(5-chloro-2-hexyl-1-methylindole-3-carbonyl)benzoic acid1464785: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assayic501.3600uM

CTD chemical–gene interactions

18 total (human), top 18 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyrenedecreases expression, increases methylation2
Tobacco Smoke Pollutiondecreases expression, increases methylation2
aristolochic acid Iincreases expression1
methyleugenoldecreases expression1
triphenyl phosphateaffects expression1
terbufosincreases methylation1
ferrous chloridedecreases expression1
perfluoro-n-nonanoic aciddecreases expression1
clothianidindecreases expression1
eprenetapoptaffects expression, affects reaction1
Allergensincreases expression1
Fonofosincreases methylation1
Parathionincreases methylation1
Tetrachlorodibenzodioxinaffects expression1
Valproic Acidincreases methylation1
Cyclosporinedecreases methylation1
Sodium Selenitedecreases expression1
Okadaic Aciddecreases expression1

ChEMBL screening assays

29 unique, capped per target: 22 functional, 7 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1686896FunctionalAgonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization at 100 nM in presence of 5-oxo-ETE5-oxo-15-HETE: total synthesis and bioactivity. — Bioorg Med Chem Lett
CHEMBL3117762BindingAntagonist activity at OXE receptor (unknown origin) expressed in neutrophils assessed as inhibition of 5-oxo-ETE-induced cell migration after 2 hrs by hematoxylin/chromotrope 2R staining-based microscopic analysisInhibition of 5-oxo-6,8,11,14-eicosatetraenoic acid-induced activation of neutrophils and eosinophils by novel indole OXE receptor antagonists. — J Med Chem

Cellosaurus cell lines

4 cell lines: 3 spontaneously immortalized cell line, 1 cancer cell line

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

CellosaurusNameCategorySex
CVCL_H489CHO-K1/Galpha15/OXER1Spontaneously immortalized cell lineFemale
CVCL_KV63cAMP Hunter CHO-K1 OXER1 GiSpontaneously immortalized cell lineFemale
CVCL_KY71PathHunter CHO-K1 OXER1 beta-arrestinSpontaneously immortalized cell lineFemale
CVCL_LB03PathHunter U2OS OXER1 Total GPCR InternalizationCancer cell lineFemale

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.