OXER1
gene geneOn this page
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
| Field | Value |
|---|---|
| HGNC ID | HGNC:24884 |
| Approved symbol | OXER1 |
| Name | oxoeicosanoid receptor 1 |
| Location | 2p21 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GPCR, TG1019, GPR170 |
| Ensembl gene | ENSG00000162881 |
| Ensembl biotype | protein_coding |
| OMIM | 620064 |
| Entrez | 165140 |
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
| Exon | Start | End |
|---|---|---|
| ENSE00001478276 | 42762499 | 42764135 |
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 ID | TPM avg | Samples expressed |
|---|---|---|
| 28023 | 0.5619 | 122 |
| 28021 | 0.1072 | 51 |
| 28022 | 0.0553 | 23 |
Top tissues by expression
243 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right lobe of liver | UBERON:0001114 | 90.79 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 84.89 | gold quality |
| liver | UBERON:0002107 | 78.93 | gold quality |
| blood | UBERON:0000178 | 78.39 | gold quality |
| right ovary | UBERON:0002118 | 77.05 | gold quality |
| granulocyte | CL:0000094 | 76.87 | gold quality |
| left ovary | UBERON:0002119 | 76.65 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 76.15 | gold quality |
| leukocyte | CL:0000738 | 75.40 | gold quality |
| monocyte | CL:0000576 | 75.20 | gold quality |
| small intestine | UBERON:0002108 | 74.27 | gold quality |
| body of pancreas | UBERON:0001150 | 73.81 | gold quality |
| ascending aorta | UBERON:0001496 | 71.97 | gold quality |
| thoracic aorta | UBERON:0001515 | 71.70 | gold quality |
| ovary | UBERON:0000992 | 71.62 | gold quality |
| metanephros cortex | UBERON:0010533 | 71.45 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 71.25 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 71.14 | gold quality |
| bone marrow cell | CL:0002092 | 70.56 | gold quality |
| endocervix | UBERON:0000458 | 70.21 | gold quality |
| mucosa of stomach | UBERON:0001199 | 70.15 | gold quality |
| ectocervix | UBERON:0012249 | 69.91 | gold quality |
| transverse colon | UBERON:0001157 | 69.71 | gold quality |
| body of uterus | UBERON:0009853 | 69.71 | gold quality |
| cortex of kidney | UBERON:0001225 | 69.64 | gold quality |
| spleen | UBERON:0002106 | 69.37 | gold quality |
| right coronary artery | UBERON:0001625 | 68.96 | gold quality |
| bone marrow | UBERON:0002371 | 68.67 | gold quality |
| sural nerve | UBERON:0015488 | 68.58 | gold quality |
| aorta | UBERON:0000947 | 68.43 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.89 |
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):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3202 | 99.66 | 67.70 | 2737 |
| HSA-MIR-6727-3P | 99.49 | 65.92 | 1333 |
| HSA-MIR-4722-3P | 99.35 | 65.22 | 1099 |
| HSA-MIR-6780B-3P | 99.13 | 67.18 | 622 |
| HSA-MIR-9500 | 98.62 | 66.54 | 1845 |
| HSA-MIR-6801-3P | 98.04 | 64.64 | 805 |
| HSA-MIR-4303 | 98.01 | 68.13 | 2304 |
| HSA-MIR-6810-3P | 97.96 | 64.57 | 1023 |
| HSA-MIR-3690 | 96.44 | 65.18 | 737 |
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
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | hcar1-3 | ENSDARG00000062874 |
| danio_rerio | hcar1-4 | ENSDARG00000087084 |
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 1 — Q8TDS5 (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)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR051893 | HCARs | Family |
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)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q8TDS5-F1 | 82.24 | 0.47 |
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
| ID | Pathway |
|---|---|
| R-HSA-391903 | Eicosanoid ligand-binding receptors |
| R-HSA-418594 | G 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:
| Category | Pathways |
|---|---|
| Class A/1 (Rhodopsin-like receptors) | 1 |
| GPCR downstream signalling | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| long-chain fatty acid binding | 3 |
| icosanoid binding | 3 |
| fatty acid derivative binding | 2 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase inhibitor activity | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
508 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| OXER1 | GPRC6A | Q5T6X5 | 622 |
| OXER1 | SLC39A9 | Q9NUM3 | 621 |
| OXER1 | LTB4R2 | Q9NPC1 | 513 |
| OXER1 | ALOX5 | P09917 | 507 |
| OXER1 | TRPM8 | Q7Z2W7 | 398 |
| OXER1 | GPR148 | Q8TDV2 | 380 |
| OXER1 | ALOX5AP | P20292 | 348 |
| OXER1 | OR4D1 | Q15615 | 320 |
| OXER1 | NPB | Q8NG41 | 312 |
| OXER1 | OR2A14 | Q96R47 | 312 |
| OXER1 | TAS2R4 | Q9NYW5 | 300 |
| OXER1 | ZNF786 | Q8N393 | 297 |
| OXER1 | ALOX12 | P18054 | 270 |
| OXER1 | ZNF30 | P17039 | 268 |
| OXER1 | MRGPRD | Q8TDS7 | 267 |
| OXER1 | TRHR | P34981 | 267 |
IntAct
135 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| LASP1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RECK | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | ASB13 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | TFG | psi-mi:“MI:0915”(physical association) | 0.560 |
| PRR20D | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| EFCAB3 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KRTAP19-5 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CRYBA2 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TP53BP1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TLE5 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | PLSCR4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | ANAPC11 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | RNF38 | psi-mi:“MI:0915”(physical association) | 0.560 |
| JMJD7 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| ZIC1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | ZC3H10 | psi-mi:“MI:0915”(physical association) | 0.560 |
| HNF1B | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OTX1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CCNK | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FOXH1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RNF44 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| VGLL3 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| HNRNPH1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | KRTAP4-2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PRKAB2 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PROP1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| OXER1 | RAMAC | psi-mi:“MI:0915”(physical association) | 0.560 |
| ESRP1 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| INTS11 | OXER1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KRTAP12-3 | OXER1 | psi-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.
| A | Effect | B | Mechanism |
|---|---|---|---|
| “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:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Keratinization | 5 | 9.3× | 9e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
109 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 97 |
| Likely benign | 9 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 59144 | GRCh38/hg38 2p21(chr2:41999414-42915744)x3 | Pathogenic |
SpliceAI
69 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:42763597:C:CT | donor_gain | 0.8300 |
| 2:42763598:C:CT | donor_gain | 0.8200 |
| 2:42763593:TGCAC:T | donor_gain | 0.6800 |
| 2:42763596:A:AC | donor_gain | 0.6300 |
| 2:42763599:A:AA | donor_gain | 0.4800 |
| 2:42763462:AGCTG:A | acceptor_gain | 0.4700 |
| 2:42764104:TTC:T | donor_gain | 0.4600 |
| 2:42764105:TCT:T | donor_gain | 0.4600 |
| 2:42763268:G:GT | acceptor_gain | 0.4500 |
| 2:42763269:T:TT | acceptor_gain | 0.4500 |
| 2:42763595:CA:C | donor_gain | 0.4500 |
| 2:42763579:G:C | donor_gain | 0.4000 |
| 2:42763543:C:CT | donor_gain | 0.3400 |
| 2:42763463:GCT:G | acceptor_gain | 0.3300 |
| 2:42763818:G:GC | acceptor_gain | 0.3300 |
| 2:42763572:CGG:C | donor_gain | 0.3200 |
| 2:42763362:A:AC | donor_gain | 0.3100 |
| 2:42763363:C:CC | donor_gain | 0.3100 |
| 2:42763583:G:C | donor_gain | 0.3100 |
| 2:42763594:GCACC:G | donor_gain | 0.3100 |
| 2:42763815:CGCG:C | acceptor_gain | 0.3100 |
| 2:42763818:G:C | acceptor_gain | 0.3100 |
| 2:42763911:A:T | acceptor_gain | 0.3000 |
| 2:42762661:G:A | donor_gain | 0.2900 |
| 2:42763279:C:CT | donor_gain | 0.2900 |
| 2:42763267:TG:T | acceptor_gain | 0.2800 |
| 2:42763814:CCGCG:C | acceptor_gain | 0.2800 |
| 2:42763317:G:A | donor_gain | 0.2700 |
| 2:42763456:C:CA | acceptor_gain | 0.2600 |
| 2:42763544:C:CT | donor_gain | 0.2600 |
AlphaMissense
2705 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:42763256:G:C | F308L | 0.982 |
| 2:42763256:G:T | F308L | 0.982 |
| 2:42763258:A:G | F308L | 0.982 |
| 2:42763247:G:C | S311R | 0.979 |
| 2:42763247:G:T | S311R | 0.979 |
| 2:42763249:T:G | S311R | 0.979 |
| 2:42763781:G:C | S133R | 0.977 |
| 2:42763781:G:T | S133R | 0.977 |
| 2:42763783:T:G | S133R | 0.977 |
| 2:42763136:A:C | S348R | 0.975 |
| 2:42763136:A:T | S348R | 0.975 |
| 2:42763138:T:G | S348R | 0.975 |
| 2:42763706:C:A | W158C | 0.973 |
| 2:42763706:C:G | W158C | 0.973 |
| 2:42763766:G:C | D138E | 0.970 |
| 2:42763766:G:T | D138E | 0.970 |
| 2:42763397:G:C | F261L | 0.960 |
| 2:42763397:G:T | F261L | 0.960 |
| 2:42763399:A:G | F261L | 0.960 |
| 2:42763169:G:C | F337L | 0.959 |
| 2:42763169:G:T | F337L | 0.959 |
| 2:42763171:A:G | F337L | 0.959 |
| 2:42763643:G:C | S179R | 0.954 |
| 2:42763643:G:T | S179R | 0.954 |
| 2:42763645:T:G | S179R | 0.954 |
| 2:42763127:G:C | D351E | 0.947 |
| 2:42763127:G:T | D351E | 0.947 |
| 2:42763847:A:C | S111R | 0.945 |
| 2:42763847:A:T | S111R | 0.945 |
| 2:42763849:T:G | S111R | 0.945 |
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):
| Study | Trait | p-value |
|---|---|---|
| GCST000278_1 | Hyperactive-impulsive symptoms | 2.000000e-06 |
| GCST000281_1 | Attention deficit hyperactivity disorder | 6.000000e-06 |
| GCST002715_2 | Breastfeeding duration | 1.000000e-06 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006864 | breastfeeding 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).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL367149 | DOCONEXENT | 3 | 63,817 |
| CHEMBL460026 | ICOSAPENT | 3 | 60,180 |
| CHEMBL465183 | DIHOMO-GAMMA-LINOLENIC ACID | 2 | 2,022 |
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:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| S‐Y048 | Antagonist | 10.7 | pIC50 |
| 5-oxo-ETE | Full agonist | 8.5 | pEC50 |
| [3H]5-oxo-ETE | Agonist | 8.4 | pKd |
| 5-oxo-C20:3 | Full agonist | 8.0 | pEC50 |
| 5-oxo-ODE | Full agonist | 8.0 | pEC50 |
| 5-oxo-15-HETE | Full agonist | 7.7 | pEC50 |
| 5S-HETE | Full agonist | 7.2 | pEC50 |
| 5S-HPETE | Full agonist | 7.0 | pEC50 |
| 5-oxo-20-HETE | Full agonist | 6.5 | pEC50 |
| 5-(6-chloro-2-hexyl-1H-indol-1-yl)-5-oxo-valeric acid | Antagonist | 6.4 | pIC50 |
| 5-oxo-12-HETE | Antagonist | 6.3 | pIC50 |
| Gue1654 | Negative | 6.0 | pIC50 |
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.
| Ligand | Measure | Value |
|---|---|---|
| (Z,Z,Z)-8,11,14-Eicosatrienoic acid | KI | 3700 nM |
| 5,8,11,14,17-EICOSAPENTAENOIC ACID | KI | 6000 nM |
ChEMBL bioactivities
84 potent at pChembl≥5 of 91 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.92 | IC50 | 0.12 | nM | CHEMBL4283608 |
| 9.55 | IC50 | 0.28 | nM | CHEMBL4287941 |
| 9.42 | IC50 | 0.38 | nM | CHEMBL4281149 |
| 8.68 | IC50 | 2.1 | nM | CHEMBL4282356 |
| 8.66 | IC50 | 2.2 | nM | CHEMBL3341973 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL3341971 |
| 8.52 | IC50 | 3 | nM | 5-OXO-ETE |
| 8.22 | IC50 | 6 | nM | CHEMBL3115775 |
| 8.22 | IC50 | 6 | nM | CHEMBL3341972 |
| 8.15 | IC50 | 7 | nM | CHEMBL3115774 |
| 8.15 | EC50 | 7 | nM | 5-OXO-ETE |
| 8.12 | IC50 | 7.5 | nM | CHEMBL1760545 |
| 7.96 | IC50 | 11 | nM | CHEMBL4284672 |
| 7.92 | IC50 | 12 | nM | CHEMBL4277299 |
| 7.80 | IC50 | 16 | nM | CHEMBL3115775 |
| 7.77 | IC50 | 17 | nM | CHEMBL3115775 |
| 7.77 | IC50 | 17 | nM | CHEMBL3115774 |
| 7.75 | IC50 | 18 | nM | CHEMBL3115774 |
| 7.75 | IC50 | 18 | nM | CHEMBL4291346 |
| 7.64 | IC50 | 23 | nM | CHEMBL4084871 |
| 7.64 | IC50 | 23 | nM | CHEMBL4291464 |
| 7.58 | IC50 | 26 | nM | CHEMBL3115793 |
| 7.55 | IC50 | 28 | nM | CHEMBL3115775 |
| 7.55 | IC50 | 28 | nM | CHEMBL3115774 |
| 7.52 | IC50 | 30 | nM | CHEMBL3115774 |
| 7.52 | IC50 | 30 | nM | CHEMBL3115786 |
| 7.48 | IC50 | 33 | nM | CHEMBL3115775 |
| 7.42 | IC50 | 38 | nM | CHEMBL4278772 |
| 7.42 | IC50 | 38 | nM | CHEMBL4279605 |
| 7.25 | EC50 | 56 | nM | CHEMBL1682258 |
| 7.17 | EC50 | 67 | nM | 5-OXO-ETE |
| 7.09 | IC50 | 81 | nM | CHEMBL3115792 |
| 7.05 | IC50 | 90 | nM | CHEMBL3115782 |
| 6.92 | IC50 | 120 | nM | CHEMBL4277207 |
| 6.87 | IC50 | 136 | nM | CHEMBL3115783 |
| 6.85 | IC50 | 141 | nM | CHEMBL3115785 |
| 6.68 | IC50 | 210 | nM | CHEMBL4280693 |
| 6.66 | EC50 | 220 | nM | 5-OXO-ETE |
| 6.65 | IC50 | 223 | nM | CHEMBL4287509 |
| 6.58 | IC50 | 260 | nM | CHEMBL4285167 |
| 6.50 | IC50 | 314 | nM | CHEMBL3115791 |
| 6.49 | IC50 | 323 | nM | CHEMBL3115787 |
| 6.42 | EC50 | 380 | nM | CHEMBL4127146 |
| 6.40 | IC50 | 400 | nM | CHEMBL2332562 |
| 6.40 | IC50 | 402 | nM | CHEMBL3115774 |
| 6.34 | IC50 | 454 | nM | CHEMBL3115775 |
| 6.34 | IC50 | 460 | nM | CHEMBL3311230 |
| 6.30 | IC50 | 500 | nM | CHEMBL3115778 |
| 6.30 | IC50 | 500 | nM | CHEMBL1526258 |
| 6.26 | IC50 | 550 | nM | CHEMBL3115800 |
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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (3S)-5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0001 | uM |
| 5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0003 | uM |
| (3S)-5-[5-chloro-2-[(1S)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0004 | uM |
| 5-[6-chloro-2-(5-phenylpentyl)indol-1-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0021 | uM |
| (3S)-5-(6-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assay | ic50 | 0.0022 | uM |
| (3R)-5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assay | ic50 | 0.0027 | uM |
| (6E,8Z,11Z,14Z)-5-oxoicosa-6,8,11,14-tetraenoic acid | 590219: Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization | ic50 | 0.0030 | uM |
| (3S)-5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1185137: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of calcium mobilization by fluorescence assay | ic50 | 0.0060 | uM |
| 5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0060 | uM |
| 5-(6-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0070 | uM |
| (6E,8Z,11Z,14Z)-20,20,20-trifluoro-5-oxoicosa-6,8,11,14-tetraenoic acid | 590219: Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization | ic50 | 0.0075 | uM |
| 5-[5-chloro-1-methyl-2-(5-phenylpentyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0110 | uM |
| 5-[6-chloro-2-(6-phenylhexyl)indol-1-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0120 | uM |
| 5-[6-chloro-2-(4-phenylbutyl)indol-1-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0180 | uM |
| (3R)-5-[5-chloro-1-methyl-2-(6-phenylhexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0230 | uM |
| 5-(5-chloro-1-methyl-2-undecylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1464785: 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 assay | ic50 | 0.0230 | uM |
| 5-(5-bromo-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0260 | uM |
| 5-(6-bromo-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0300 | uM |
| 5-[5-chloro-1-methyl-2-(4-phenylbutyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0380 | uM |
| 5-[5-chloro-1-methyl-2-(6,6,6-trifluorohexyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.0380 | uM |
| (6E,8Z,11Z,13E,15S)-15-hydroxy-5-oxoicosa-6,8,11,13-tetraenoic acid | 579486: Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization | ec50 | 0.0560 | uM |
| 5-(6-chloro-2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0810 | uM |
| 5-(2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.0900 | uM |
| (3R)-5-[5-chloro-2-[(1S)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.1200 | uM |
| 5-(2-hexyl-3-methylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.1360 | uM |
| 5-(5-chloro-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.1410 | uM |
| 5-[6-chloro-2-(3-phenylpropyl)indol-1-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.2100 | uM |
| 5-[5-chloro-1-methyl-2-(3-phenylpropyl)indol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.2230 | uM |
| (3S)-5-[5-chloro-2-[(1R)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.2600 | uM |
| 5-(2-hexyl-1-methylindol-3-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.3140 | uM |
| 5-(2-hexyl-6-methoxyindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.3230 | uM |
| (6E,8Z,11Z,14Z,17Z)-5-oxoicosa-6,8,11,14,17-pentaenoic acid | 1497846: Agonist activity at human PK-tagged OXER1 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation assay | ec50 | 0.3800 | uM |
| 5-(6-chloroindol-1-yl)-5-oxopentanoic acid | 736229: 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 analysis | ic50 | 0.4000 | uM |
| 5-[6-chloro-2-[(Z)-hex-1-enyl]indol-1-yl]-3-methyl-5-oxopentanoic acid | 1180185: 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 spectrofluorometry | ic50 | 0.4600 | uM |
| (6E,8Z,10E,12S,14Z)-12-hydroxy-5-oxoicosa-6,8,10,14-tetraenoic acid | 1067794: Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization by spectrofluorometric analysis | ic50 | 0.5000 | uM |
| (5Z,8Z,10E,12S,14Z)-12-hydroxyicosa-5,8,10,14-tetraenoic acid | 1410868: 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 assay | ic50 | 0.5000 | uM |
| 5-oxo-5-[2-[(Z)-undec-1-enyl]indol-1-yl]pentanoic acid | 1067795: 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 analysis | ic50 | 0.5500 | uM |
| 5-(5-chloro-2-hexyl-1-methylindol-3-yl)-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.5660 | uM |
| 5-(2-octylindol-1-yl)-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.5700 | uM |
| 2-[1-[2-(5-chloro-2-hexyl-1-methylindol-3-yl)-2-oxoethyl]cyclopropyl]acetic acid | 1464785: 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 assay | ic50 | 0.5800 | uM |
| 5-(5-bromo-2-hexylindol-1-yl)-3-methyl-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.6380 | uM |
| 5-oxo-5-(2-undecylindol-1-yl)pentanoic acid | 1067795: 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 analysis | ic50 | 0.7000 | uM |
| 2-[1-[2-(5-chloro-2-hexyl-1-methylindol-3-yl)-2-oxoethyl]cyclobutyl]acetic acid | 1464785: 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 assay | ic50 | 0.7200 | uM |
| (3R)-5-[5-chloro-2-[(1R)-1-hydroxy-6-phenylhexyl]-1-methylindol-3-yl]-3-methyl-5-oxopentanoic acid | 1410867: 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 assay | ic50 | 0.7500 | uM |
| 5-(2-heptylindol-1-yl)-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 0.7500 | uM |
| 3-(5-chloro-2-hexyl-1-methylindole-3-carbonyl)benzoic acid | 1464785: 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 assay | ic50 | 1.1200 | uM |
| 5-(2-hexylindol-1-yl)-5-oxopentanoic acid | 1067795: 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 analysis | ic50 | 1.1300 | uM |
| 5-(5-chloroindol-1-yl)-5-oxopentanoic acid | 736229: 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 analysis | ic50 | 1.1700 | uM |
| 5-(5-chloro-2-hexyl-1-methylindol-3-yl)-3,3-dimethyl-5-oxopentanoic acid | 1464785: 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 assay | ic50 | 1.3300 | uM |
| 4-(5-chloro-2-hexyl-1-methylindole-3-carbonyl)benzoic acid | 1464785: 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 assay | ic50 | 1.3600 | uM |
CTD chemical–gene interactions
18 total (human), top 18 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | decreases expression, increases methylation | 2 |
| Tobacco Smoke Pollution | decreases expression, increases methylation | 2 |
| aristolochic acid I | increases expression | 1 |
| methyleugenol | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| terbufos | increases methylation | 1 |
| ferrous chloride | decreases expression | 1 |
| perfluoro-n-nonanoic acid | decreases expression | 1 |
| clothianidin | decreases expression | 1 |
| eprenetapopt | affects expression, affects reaction | 1 |
| Allergens | increases expression | 1 |
| Fonofos | increases methylation | 1 |
| Parathion | increases methylation | 1 |
| Tetrachlorodibenzodioxin | affects expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Cyclosporine | decreases methylation | 1 |
| Sodium Selenite | decreases expression | 1 |
| Okadaic Acid | decreases expression | 1 |
ChEMBL screening assays
29 unique, capped per target: 22 functional, 7 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1686896 | Functional | Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization at 100 nM in presence of 5-oxo-ETE | 5-oxo-15-HETE: total synthesis and bioactivity. — Bioorg Med Chem Lett |
| CHEMBL3117762 | Binding | Antagonist 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 analysis | Inhibition 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):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_H489 | CHO-K1/Galpha15/OXER1 | Spontaneously immortalized cell line | Female |
| CVCL_KV63 | cAMP Hunter CHO-K1 OXER1 Gi | Spontaneously immortalized cell line | Female |
| CVCL_KY71 | PathHunter CHO-K1 OXER1 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_LB03 | PathHunter U2OS OXER1 Total GPCR Internalization | Cancer cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.