LTB4R2

Summary

LTB4R2 (leukotriene B4 receptor 2, HGNC:19260) is a protein-coding gene on chromosome 14q12, encoding Leukotriene B4 receptor 2 (Q9NPC1). Low-affinity receptor for leukotrienes including leukotriene B4. It is a selective cancer dependency (DepMap: 83.9% of cell lines).

Predicted to enable G protein-coupled peptide receptor activity and leukotriene B4 receptor activity. Predicted to be involved in neuropeptide signaling pathway. Predicted to act upstream of or within keratinocyte migration and signal transduction. Located in nucleoplasm and plasma membrane.

Source: NCBI Gene 56413 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 124 total
• Druggable target: yes — 6 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 83.9% of screened cell lines
• MANE Select transcript: NM_019839

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19260
Approved symbol	LTB4R2
Name	leukotriene B4 receptor 2
Location	14q12
Locus type	gene with protein product
Status	Approved
Aliases	BLTR2, BLT2, JULF2, NOP9
Ensembl gene	ENSG00000213906
Ensembl biotype	protein_coding
OMIM	605773
Entrez	56413

Gene structure

Transcript identifiers

Ensembl transcripts: 5 — 5 protein_coding

ENST00000527924, ENST00000528054, ENST00000530080, ENST00000533293, ENST00000543919

RefSeq mRNA: 2 — MANE Select: NM_019839 NM_001164692, NM_019839

CCDS: CCDS9625

Canonical transcript exons

ENST00000533293 — 2 exons

Exon	Start	End
ENSE00002154078	24310140	24310255
ENSE00002172199	24310655	24312038

Expression profiles

Bgee: expression breadth ubiquitous, 131 present calls, max score 90.02.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.8605 / max 117.6566, expressed in 180 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139028	0.5868	84
139030	0.1851	90
139029	0.0886	43

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
skin of abdomen	UBERON:0001416	90.02	gold quality
esophagus mucosa	UBERON:0002469	89.77	gold quality
zone of skin	UBERON:0000014	89.51	gold quality
skin of leg	UBERON:0001511	89.23	gold quality
lower esophagus mucosa	UBERON:0035834	86.40	gold quality
granulocyte	CL:0000094	84.47	gold quality
monocyte	CL:0000576	82.91	gold quality
vagina	UBERON:0000996	82.91	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	82.26	gold quality
leukocyte	CL:0000738	82.19	gold quality
blood	UBERON:0000178	80.60	gold quality
spleen	UBERON:0002106	80.18	gold quality
sural nerve	UBERON:0015488	80.04	gold quality
esophagus	UBERON:0001043	79.32	gold quality
minor salivary gland	UBERON:0001830	79.06	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	78.30	gold quality
saliva-secreting gland	UBERON:0001044	77.80	gold quality
right uterine tube	UBERON:0001302	77.37	gold quality
bone marrow	UBERON:0002371	77.29	gold quality
ectocervix	UBERON:0012249	76.23	gold quality
adrenal tissue	UBERON:0018303	76.03	gold quality
bone marrow cell	CL:0002092	75.16	gold quality
left adrenal gland cortex	UBERON:0035825	75.15	gold quality
mucosa of stomach	UBERON:0001199	74.80	gold quality
left adrenal gland	UBERON:0001234	74.78	gold quality
stromal cell of endometrium	CL:0002255	74.40	gold quality
right adrenal gland	UBERON:0001233	74.38	gold quality
uterine cervix	UBERON:0000002	74.19	gold quality
subcutaneous adipose tissue	UBERON:0002190	74.04	gold quality
right lung	UBERON:0002167	74.02	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.72

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

15 targeting LTB4R2, 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-513B-5P	99.99	69.96	2150
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-182-5P	99.87	74.03	2589
HSA-MIR-6745	99.74	65.33	1321
HSA-MIR-363-5P	99.46	64.51	1015
HSA-MIR-196A-3P	99.19	67.34	1204
HSA-MIR-6815-3P	99.13	68.98	1530
HSA-MIR-608	98.93	67.83	2013
HSA-MIR-4443	98.02	66.25	1928
HSA-MIR-9851-5P	97.57	67.49	1067
HSA-MIR-5699-5P	97.36	67.03	1014
HSA-MIR-6515-5P	97.08	65.48	1219
HSA-MIR-4540	96.90	67.46	473
HSA-MIR-6821-3P	95.21	66.79	578
HSA-MIR-5684	93.17	64.85	454

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 83.9% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• BLT2 is a low-affinity leucotriene B4 receptor; 358 amino acid sequence is 92.7% identical to the mouse receptor (PMID:12895595)
• BLT2 (the low-affinity receptor for LTB4) showed stronger expression than BLT1 (the high-affinity receptor) in actively inflamed synovial tissue from patients with rheumatoid arthritis (PMID:12913925)
• LTB4-BLT2-linked cascade plays a crucial mediatory role in the cell transformation induced by oncogenic Ha-Ras(V12), possibly acting downstream of Rac-cPLA2 (PMID:15489890)
• Data indicate that expression of functional leukotriene B4 receptors (BLT1 and 2) may occur at the surface of endothelial cells in response to lipopolysaccharides, cytokines, and LTB4. (PMID:16624877)
• demonstrates expression of functional Leukotriene B4 receptors, both BLT1 and BLT2, in murine and human mast cells and a regulatory role for stem cell factor in their expression (PMID:16920986)
• BLT2-Nox1-linked cascade is responsible for the elevated ROS generation in Ras-transformed cells. (PMID:18082638)
• Genetic variation in leukotriene pathway members and their receptors confer an increased risk of ischemic stroke in 2 independent populations (PMID:18323512)
• BLT2 was expressed in 45% of ovarian neoplasms and correlated with advanced stage III/IV disease, suboptimal debulking, and platinum resistance. (PMID:18421027)
• Upregulation of BLT2 is already evident in precursor lesions (PanINs, IPMNs). Overexpression of this receptor leads to significant growth stimulation (PMID:18781173)
• LTB4 phosphorylates MAPKs and stimulates NF-kappaB-dependent inflammation via BLT1 and BLT2 receptors in cultured monocytic cells. The blockade of this pathway could be a novel and potential therapeutic target in atherothrombosis. (PMID:18852255)
• the response of the pleural mesothelium to LTB4 is the result of a balance between the activation of receptors for LTB4 with a proinflammatory outcome (BLT2) and the activation of a different receptor for LTB4 with an anti-inflammatory outcome (PPAR). (PMID:18981151)
• results suggest that the helix 8 region of hBLT2 plays an important role in transport-competent receptor folding. (PMID:19126593)
• Findings indicate that BLT2 plays an essential role in mediating VEGF-induced angiogenesis. (PMID:19286633)
• BLT2 plays a pivotal, mediatory role in the pathogenesis of asthma, acting through a “reactive oxygen species-NF-kappaB”-linked inflammatory signaling pathway. (PMID:19448154)
• the ‘BLT2-Nox1-ROS’-linked cascade is involved in the pro-survival signaling, especially in ER-negative breast cancer cells. (PMID:19748928)
• BLT2 stimulates the purified G alpha(i2) beta(1) gamma(2) protein more efficiently than the dimer; assembly of two BLT2 protomers into a dimer results in the reduced ability to signal (PMID:20026606)
• a “BLT2-Nox1”-linked pathway has a crucial role in UVB-induced ROS generation and mediates apoptosis in human keratinocytes (PMID:20090768)
• BLT2-Nox1-reactive oxygen species-dependent pathway plays a role in promoting the secretion of IL-8 from human mast cells in response to the proinflammatory cytokine IL-1beta, thus contributing to angiogenesis. (PMID:20194723)
• Up-regulation of BLT2 is associated with bladder cancer. (PMID:21252614)
• BLT2 phosphorylation at Thr355 by Akt is necessary for BLT2-mediated chemotaxis (PMID:22044535)
• The results suggested that LTB4 receptors BLT1 and BLT2 are involved in IL-8 production in and secretion by human neutrophils induced by T. vaginalis. (PMID:22215047)
• Leukotriene B4 receptor-2 promotes invasiveness and metastasis of ovarian cancer cells through signal transducer and activator of transcription 3 (STAT3)-dependent up-regulation of matrix metalloproteinase 2 (PMID:22396544)
• these findings point to BLT2 as a key regulator of AR expression and will contribute to the development of novel therapies for AR-positive prostate cancers, including androgen-responsive and castration-resistant prostate cancers. (PMID:22426480)
• our study demonstrates that a BLT2 up-regulates IL-8 production , thereby contributing to the invasiveness of these aggressive breast cancer cells. (PMID:23145117)
• LTB4R2 shows splice variation in the 5’-untranslated region and multiple promoter regions. LTB4R2 polymorphisms do not appear to be susceptibility markers for the development of asthma in Caucasian subjects. (PMID:23167751)
• Findings suggest that, in bronchial epithelial cells, cigarette smoke extracts (CSE) promote induction of pro-inflammatory BLT2 receptors and activate mechanisms leading to increased neutrophil adhesion. (PMID:23347335)
• Findings indicate that BLT2 has a protective role in allergic airway inflammation and that diminished BLT2 expression in CD4(+) T cells may contribute to the pathophysiology of asthma. (PMID:23603839)
• BLT2 is a novel therapeutic target that sensitises drug-resistant breast cancer cells to paclitaxel. (PMID:23799854)
• RanBPM acts as a negative regulator of BLT2 signaling to attenuate BLT2-mediated cell motility (PMID:23928309)
• BLT2-NOX-ROS-NF-kappaB cascade induction during detachment confers a novel mechanism of anoikis resistance in prostate cancer cells and potentially contributes to prostate cancer progression. (PMID:23986446)
• searched BLT2 downstream components and identified reactive oxygen species and nuclear factor kappaB as critical components that contribute to epithelial-mesenchymal transition in mammary epithelial cells (PMID:24990945)
• BLT1 and BLT2 are therefore potential targets for the development of novel drugs. (PMID:25480980)
• Authors demonstrated that MyD88 lies upstream of BLT2 in LPS-potentiated invasiveness and that this ‘MyD88-BLT2’ cascade mediates activation of NF-kappaB and the synthesis of IL-6 and IL-8 critical for the invasiveness and aggression of breast cancer cells. (PMID:25691060)
• Data show that signal transducer and activator of transcription-3 (STAT-3) activation occurs downstream of leukotriene B4 receptor-2 (BLT2) and mediates cisplatin resistance in SK-OV-3 cells. (PMID:26597704)
• BLT2 ligation facilitates F-actin assembly with the upregulated phosphorylation of MYPT1. (PMID:26896822)
• BLT2 inhibition induces apoptosis, inhibits proliferation, colony formation and self-renewal capacity of CD34(+) cells from tyrosine kinase inhibitor - resistant blast phase-chronic myeloid leukemia patients. (PMID:26966074)
• Leukotriene B4 receptor type 2 protects against pneumolysin-dependent acute lung injury. (PMID:27703200)
• RanBPM acts as a negative regulator of BLT2 and IL8, thus attenuating the invasiveness of aggressive breast cancer cells (PMID:28027932)
• Supernatants and lipids from stored red blood cells activate pulmonary microvascular endothelium through the BLT2 receptor (PMID:28880373)
• BLT2 gene polymorphism (D196G) enhances ligand sensitivity, thereby increasing cell motility in response to low-dose ligand stimulation. (PMID:29170475)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	ltb4r2b	ENSDARG00000054170
danio_rerio	ltb4r2a	ENSDARG00000088615
mus_musculus	Ltb4r2	ENSMUSG00000040432
rattus_norvegicus	Ltb4r2	ENSRNOG00000020382
drosophila_melanogaster	Rh7	FBGN0036260
caenorhabditis_elegans	trhr-1	WBGENE00016265

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Leukotriene B4 receptor 2 — Q9NPC1 (reviewed: Q9NPC1)

Alternative names: LTB4 receptor JULF2, Leukotriene B4 receptor BLT2, Seven transmembrane receptor BLTR2

All UniProt accessions (4): A0A3Q5ACI7, E9PIC1, E9PNJ6, Q9NPC1

UniProt curated annotations — full annotation on UniProt →

Function. Low-affinity receptor for leukotrienes including leukotriene B4. Mediates chemotaxis of granulocytes and macrophages. The response is mediated via G-proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTB4 > 12-epi-LTB4 > LTB5 > LTB3.

Subcellular location. Cell membrane.

Tissue specificity. Widely expressed.

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

RefSeq proteins (2): NP_001158164, NP_062813* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR003981	Leukotriene_B4_rcpt	Family
IPR003982	Leukotriene_B4_typ-2_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (20 total): topological domain 8, transmembrane region 7, compositionally biased region 2, chain 1, region of interest 1, glycosylation site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NPC1-F1	81.39	0.45

Functional residue map

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

Glycosylation sites (1): 10

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-391906	Leukotriene receptors
R-HSA-416476	G alpha (q) signalling events
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-391903	Eicosanoid ligand-binding receptors
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 149 (showing top): GSE45365_NK_CELL_VS_CD11B_DC_DN, GOBP_RIBOSOME_BIOGENESIS, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GCANCTGNY_MYOD_Q6, SHEPARD_CRASH_AND_BURN_MUTANT_UP, GOBP_MATURATION_OF_SSU_RRNA, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_AMEBOIDAL_TYPE_CELL_MIGRATION, chr14q12, MONNIER_POSTRADIATION_TUMOR_ESCAPE_UP, GOBP_NUCLEAR_TRANSPORT, GOBP_TAXIS, GOBP_REGULATION_OF_ADENYLATE_CYCLASE_ACTIVITY, GOBP_MATURATION_OF_5_8S_RRNA_FROM_TRICISTRONIC_RRNA_TRANSCRIPT_SSU_RRNA_5_8S_RRNA_LSU_RRNA, GOBP_TISSUE_MIGRATION

GO Biological Process (7): chemotaxis (GO:0006935), negative regulation of adenylate cyclase activity (GO:0007194), neuropeptide signaling pathway (GO:0007218), keratinocyte migration (GO:0051546), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), leukotriene signaling pathway (GO:0061737)

GO Molecular Function (4): leukotriene B4 receptor activity (GO:0001632), leukotriene receptor activity (GO:0004974), G protein-coupled peptide receptor activity (GO:0008528), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (3): nucleoplasm (GO:0005654), plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-6 pathways:

Category	Pathways
Signaling by GPCR	2
Eicosanoid ligand-binding receptors	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
G protein-coupled receptor activity	2
cellular anatomical structure	2
response to chemical	1
taxis	1
adenylate cyclase activity	1
negative regulation of catalytic activity	1
regulation of adenylate cyclase activity	1
epithelial cell migration	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
signal transduction	1
leukotriene receptor activity	1
icosanoid receptor activity	1
leukotriene signaling pathway	1
peptide receptor activity	1
transmembrane signaling receptor activity	1
nuclear lumen	1
membrane	1
cell periphery	1

Protein interactions and networks

STRING

524 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LTB4R2	LTA4H	P09960	892
LTB4R2	LTC4S	Q16873	870
LTB4R2	CYSLTR2	Q9NS75	772
LTB4R2	ABCC1	P33527	684
LTB4R2	ALOX5	P09917	667
LTB4R2	PTGER3	P43115	591
LTB4R2	ALOX5AP	P20292	578
LTB4R2	CYSLTR1	Q9Y271	555
LTB4R2	LTB4R	Q15722	529
LTB4R2	CCL19	Q99731	527
LTB4R2	OXER1	Q8TDS5	513
LTB4R2	PTGER1	P34995	483
LTB4R2	PLA2G4A	P47712	461
LTB4R2	PTGER4	P35408	447
LTB4R2	ALOX15	P16050	446

IntAct

51 interactions, top by confidence:

A	B	Type	Score
LTB4R2	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.400
LTB4R2	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
LTB4R2	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
AKT1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.400
AP2M1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CANX	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CSNK2B	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CTSA	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CEBPZ	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CNOT10	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CHPT1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
LAMP5	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CRELD2	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
DDOST	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
FOLR1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
GPR146	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
GPR37	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
GJC2	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
GLOD4	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
P4HTM	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
IMP4	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
IL17RD	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
TMEM94	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
CERS1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
MDH1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
MGLL	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
MYO1E	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
PER1	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370
PIGM	LTB4R2	psi-mi:“MI:0915”(physical association)	0.370

BioGRID (51): LTB4R2 (Reconstituted Complex), LTB4R2 (FRET), LTB4R2 (Biochemical Activity), LTB4R2 (Affinity Capture-RNA), AP2M1 (Two-hybrid), CANX (Two-hybrid), CSNK2B (Two-hybrid), CTSA (Two-hybrid), CEBPZ (Two-hybrid), CNOT10 (Two-hybrid), CHPT1 (Two-hybrid), LAMP5 (Two-hybrid), CRELD2 (Two-hybrid), DDOST (Two-hybrid), FOLR1 (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: A0T2N3, B9VR26, F1MV99, O00254, O08858, O09047, O42179, O55197, O62747, O77590, O88634, O88680, O88855, P0C5I1, P0C7U4, P25095, P25104, P25930, P29089, P29754, P29755, P30555, P30556, P30680, P30874, P30875, P30935, P30936, P30938, P32300, P32745, P33396, P33533, P33535, P34976, P34993, P34994, P35346, P35370, P35372

SIGNOR signaling

5 interactions.

A	Effect	B	Mechanism
AKT	unknown	LTB4R2	phosphorylation
AKT1	unknown	LTB4R2	phosphorylation
LTB4R2	“up-regulates activity”	GNAI1	binding
LTB4R2	“up-regulates activity”	GNAI3	binding
“Compound A [PMID:15866883]”	“up-regulates activity”	LTB4R2	“chemical activation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 49 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.

GO biological processes:

GO term	Partners	Fold	FDR
intracellular protein transport	7	10.3×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	107
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2236 predictions. Top by Δscore:

Variant	Effect	Δscore
14:24300494:G:GT	donor_gain	1.0000
14:24301560:T:TA	acceptor_gain	1.0000
14:24301561:G:A	acceptor_gain	1.0000
14:24301610:A:AG	acceptor_gain	1.0000
14:24301611:G:GA	acceptor_gain	1.0000
14:24301611:GAA:G	acceptor_gain	1.0000
14:24301611:GAAGC:G	acceptor_gain	1.0000
14:24301723:G:T	donor_loss	1.0000
14:24301724:T:A	donor_loss	1.0000
14:24301732:G:T	donor_gain	1.0000
14:24302230:A:AG	acceptor_gain	1.0000
14:24302231:G:GT	acceptor_gain	1.0000
14:24302231:GT:G	acceptor_gain	1.0000
14:24302231:GTC:G	acceptor_gain	1.0000
14:24302231:GTCC:G	acceptor_gain	1.0000
14:24302231:GTCCC:G	acceptor_gain	1.0000
14:24302421:GCTG:G	donor_gain	1.0000
14:24302422:CTGG:C	donor_loss	1.0000
14:24302423:TGG:T	donor_loss	1.0000
14:24302424:GGT:G	donor_loss	1.0000
14:24302425:G:GA	donor_loss	1.0000
14:24302425:G:GG	donor_gain	1.0000
14:24302426:T:A	donor_loss	1.0000
14:24303073:GCT:G	acceptor_gain	1.0000
14:24303727:TTTA:T	acceptor_loss	1.0000
14:24303728:TTA:T	acceptor_loss	1.0000
14:24303729:TA:T	acceptor_loss	1.0000
14:24303730:A:AG	acceptor_gain	1.0000
14:24303730:AG:A	acceptor_gain	1.0000
14:24303731:G:GT	acceptor_gain	1.0000

AlphaMissense

2210 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:24311010:A:C	S116R	0.996
14:24311012:C:A	S116R	0.996
14:24311012:C:G	S116R	0.996
14:24311508:A:C	S282R	0.996
14:24311510:C:A	S282R	0.996
14:24311510:C:G	S282R	0.996
14:24311502:A:C	S280R	0.995
14:24311504:T:A	S280R	0.995
14:24311504:T:G	S280R	0.995
14:24310925:G:C	W87C	0.994
14:24310925:G:T	W87C	0.994
14:24310986:A:C	S108R	0.994
14:24310988:C:A	S108R	0.994
14:24310988:C:G	S108R	0.994
14:24311361:T:C	F233L	0.994
14:24311363:C:A	F233L	0.994
14:24311363:C:G	F233L	0.994
14:24310944:T:A	C94S	0.992
14:24310945:G:C	C94S	0.992
14:24310974:A:C	S104R	0.992
14:24310976:C:A	S104R	0.992
14:24310976:C:G	S104R	0.992
14:24311512:T:A	V283D	0.992
14:24311516:C:A	N284K	0.992
14:24311516:C:G	N284K	0.992
14:24311518:C:A	P285Q	0.992
14:24310765:G:A	G34E	0.991
14:24311232:T:C	F190L	0.991
14:24311234:C:A	F190L	0.991
14:24311234:C:G	F190L	0.991

dbSNP variants (sampled 300 via entrez): RS1000076387 (14:24308808 C>A), RS1000519268 (14:24309126 A>C), RS1001512399 (14:24310053 C>T), RS1001777583 (14:24312013 T>A,C), RS1001807949 (14:24308372 A>G), RS1004288668 (14:24310888 C>T), RS1005027728 (14:24309682 T>A), RS1006376664 (14:24312431 G>A,C), RS1008189724 (14:24310136 C>G,T), RS1008385732 (14:24310133 C>T), RS1008663130 (14:24310411 G>A), RS1008936489 (14:24309872 C>CA), RS1009611603 (14:24311147 C>A), RS1010640382 (14:24309130 T>C), RS1011546003 (14:24312125 G>A,C)

Disease associations

OMIM: gene MIM:605773 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST008163_14	Height	4.000000e-06
GCST010206_7	Anorectal malformation	4.000000e-16

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2095160 (PROTEIN FAMILY), CHEMBL3191 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 109,418 (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
CHEMBL1069	VALSARTAN	4	38,585
CHEMBL1513	IRBESARTAN	4	31,667
CHEMBL1016	CANDESARTAN	3	37,149
CHEMBL22016	ABLUKAST	2	1,780
CHEMBL301829	CP-195543	2	83
CHEMBL329123	ETALOCIB	2	154

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 (10 total), top 10:

Ligand	Action	Affinity	Parameter
[3H]LTB4		9.7	pKd
12-hydroxyheptadecatrienoic acid	Full agonist	7.72	pEC50
CAY10583	Full agonist	7.7	pEC50
15S-HETE	Partial agonist	7.52	pEC50
12-epi LTB4	Partial agonist	7.52	pEC50
12S-HETE	Partial agonist	7.52	pEC50
LY255283	Antagonist	7.1	pIC50
LTB4	Partial agonist	6.85	pEC50
ZK-158252	Antagonist	6.0	pIC50
CP-195543	Partial agonist	5.0	pEC50

Binding affinities (BindingDB)

30 measured of 42 human assays (46 total across all organisms); most potent 30 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate	KI	0.26 nM
LTB4-20-hydroxy	KI	0.54 nM
5,12-Dihete	KI	0.7 nM
NSC_5311297	KI	2.3 nM
NSC_5283125	KI	3.7 nM
LTB4-3-aminopropylamide	KI	5.1 nM
CAS_5280876	KI	7.6 nM
NSC_1589	KI	13 nM
(Z)-3-{3-(2-Carboxy-ethyl)-4-[6-(4-methoxy-phenyl)-hex-5-enyloxy]-benzoyl}-benzoic acid	KI	15 nM
LTB4-20-carboxy	KI	20 nM
CGS 23130	KI	24 nM
(5R)-6-[6-[(1E,3S,5Z)-3-hydroxyundeca-1,5-dienyl]pyridin-2-yl]hexane-1,5-diol	KI	25 nM
LTB4-14,15-dehydro	KI	27 nM
LY 255283	KI	116 nM
CGS 23113	KI	124 nM
CGS 24115	KI	131 nM
NSC_128572	KI	190 nM
CGS 23167	KI	293 nM
LTB4-6-trans	KI	336 nM
CGS 23114	KI	885 nM
HETE-5(S)	KI	1000 nM
ETE-5-Oxo	KI	1000 nM
SR 147778	KI	1000 nM
NSC_1777	KI	1000 nM
NSC_5283162	KI	1000 nM
ONO 4057	KI	1200 nM
NSC_5280914	KI	1440 nM
CAS_103177-37-3	KI	3620 nM
LTA3-ME	KI	5000 nM
NSC_5283124	KI	5700 nM

ChEMBL bioactivities

708 potent at pChembl≥5 of 745 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.40	Ki	0.04	nM	CHEMBL292782
9.96	Ki	0.11	nM	CHEMBL340460
9.92	Ki	0.12	nM	LEUKOTRIENE_B4
9.78	EC50	0.166	nM	CHEMBL4637519
9.77	EC50	0.17	nM	CHEMBL4637519
9.44	IC50	0.36	nM	CHEMBL328712
9.35	IC50	0.45	nM	CHEMBL125723
9.33	Ki	0.47	nM	CHEMBL292782
9.29	EC50	0.51	nM	CHEMBL5724552
9.29	EC50	0.5129	nM	CHEMBL5724552
9.24	IC50	0.58	nM	CHEMBL125646
9.24	Ki	0.57	nM	CHEMBL340460
9.22	IC50	0.6	nM	CHEMBL126200
9.15	Ki	0.71	nM	CHEMBL136700
9.10	IC50	0.8	nM	CHEMBL125214
9.00	Ki	1	nM	CHEMBL95525
9.00	Ki	1	nM	CHEMBL86900
9.00	Ki	1	nM	MOXILUBANT MALEATE
9.00	Ki	1	nM	CHEMBL420075
9.00	Ki	1	nM	CHEMBL5428366
9.00	IC50	1	nM	CHEMBL125559
9.00	IC50	1	nM	CHEMBL333493
9.00	IC50	1	nM	CHEMBL341116
9.00	Ki	1	nM	CHEMBL95453
9.00	Ki	1	nM	CHEMBL98718
8.97	IC50	1.07	nM	CHEMBL123486
8.96	IC50	1.1	nM	CHEMBL5639788
8.92	IC50	1.2	nM	CHEMBL292782
8.92	IC50	1.2	nM	CHEMBL5640036
8.92	Ki	1.2	nM	CHEMBL88337
8.89	Ki	1.3	nM	CHEMBL419948
8.89	IC50	1.3	nM	CHEMBL122852
8.85	EC50	1.4	nM	CHEMBL4632597
8.85	EC50	1.413	nM	CHEMBL4632597
8.85	Ki	1.4	nM	CHEMBL139969
8.85	Ki	1.4	nM	CHEMBL336469
8.84	IC50	1.45	nM	CHEMBL3706723
8.82	IC50	1.5	nM	CHEMBL332813
8.82	IC50	1.5	nM	CHEMBL419419
8.82	IC50	1.5	nM	CHEMBL127340
8.82	IC50	1.5	nM	CHEMBL341360
8.74	IC50	1.8	nM	CHEMBL129463
8.72	IC50	1.9	nM	LEUKOTRIENE_B4
8.72	Ki	1.9	nM	LEUKOTRIENE_B4
8.70	Ki	2	nM	CHEMBL96023
8.70	Ki	2	nM	CHEMBL96004
8.70	IC50	2	nM	CP-195543
8.70	Ki	2	nM	CHEMBL328712
8.70	IC50	2	nM	CHEMBL5639897
8.70	IC50	2	nM	CHEMBL125476

PubChem BioAssay actives

523 with measured affinity, of 828 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
5-(2-carboxyethyl)-6-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-9-oxoxanthene-2-carboxylic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	<0.0001	uM
5-(2-carboxyethyl)-6-[3-(2-ethyl-5-hydroxy-4-phenylphenoxy)propoxy]-9-oxoxanthene-2-carboxylic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0001	uM
(5S,6Z,8E,10E,12R,14Z)-5,12-dihydroxyicosa-6,8,10,14-tetraenoic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0001	uM
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylnaphthalene-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0004	uM
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalene-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0004	uM
(E)-3-[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalen-2-yl]prop-2-enoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0006	uM
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-pentoxynaphthalene-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0006	uM
5-[2-(2-carboxyethyl)-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]phenyl]pentanoic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0007	uM
(2E)-2-[[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalen-2-yl]methylidene]butanoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0008	uM
(E)-3-[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindol-3-yl]prop-2-enoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0010	uM
(E)-3-[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylnaphthalen-2-yl]prop-2-enoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0010	uM
(2E,4E)-5-[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalen-2-yl]penta-2,4-dienoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0010	uM
5-[2-(2-carboxyethyl)-3-[6-(2-propylphenoxy)hexyl]phenoxy]pentanoic acid	2009629: Antagonist activity against LTB4 receptor (unknown origin) assessed as inhibition constant	ki	0.0010	uM
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-7-phenylmethoxynaphthalene-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0011	uM
(E)-3-[4-[4-[(3-fluoro-N-pentanoylanilino)methyl]phenyl]phenoxy]prop-2-enoic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0011	uM
4-[4-[(3-fluoro-N-pentanoylanilino)methyl]phenyl]benzoic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0012	uM
6-[3-(4-acetyl-2-ethyl-5-hydroxyphenoxy)propoxy]-5-(2-carboxyethyl)-9-oxoxanthene-2-carboxylic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0012	uM
(2E)-2-[[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-5-phenylmethoxyindol-3-yl]methylidene]butanoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0013	uM
3-[(2S)-7-[3-[2-(cyclopropylmethyl)-3-methoxy-4-(methylcarbamoyl)phenoxy]propoxy]-8-propyl-3,4-dihydro-2H-chromen-2-yl]propanoic acid	2009629: Antagonist activity against LTB4 receptor (unknown origin) assessed as inhibition constant	ki	0.0013	uM
1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindole-3-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0014	uM
2-[3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-2-propylphenyl]sulfinylbenzoic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0014	uM
3-[2-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-6-[4-(2H-tetrazol-5-yl)butyl]phenyl]propanoic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0014	uM
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenoxynaphthalene-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0015	uM
1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-5-phenylmethoxyindole-3-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0015	uM
(2E)-2-[[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindol-3-yl]methylidene]butanoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0015	uM
(2E,4E)-5-[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindol-3-yl]penta-2,4-dienoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0015	uM
3-[3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-9-oxoxanthen-4-yl]propanoic acid	147536: Inhibition of LTB4-induced up-regulation of human neutrophil CD11b/CD18 integrin	ic50	0.0018	uM
(E)-3-[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenoxynaphthalen-2-yl]prop-2-enoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0020	uM
2-[4-[4-[(3-methyl-N-pentanoylanilino)methyl]phenyl]phenoxy]acetic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0020	uM
2-[(3S,4R)-3-benzyl-4-hydroxy-3,4-dihydro-2H-chromen-7-yl]-4-(trifluoromethyl)benzoic acid	90993: Ability to inhibit LTB4-induced chemotaxis of isolated human neutrophils.	ic50	0.0020	uM
2-[4-[4-[[N-pentanoyl-3-(trifluoromethyl)anilino]methyl]phenyl]phenoxy]acetic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0021	uM
(E)-3-[5-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-2-phenylmethoxyphenyl]prop-2-enoic acid	99773: Binding affinity for Leukotriene B4 receptor of guinea pig spleen membranes	ic50	0.0023	uM
(E)-2-methyl-3-[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindol-3-yl]prop-2-enoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0023	uM
1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-5-phenylmethoxyindole-2-carboxylic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0025	uM
2-[3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-2-propylphenoxy]-6-fluorobenzoic acid	91333: Inhibition of LTB4 induced expression of human neutrophil integrin CD11b/CD18.	ic50	0.0025	uM
2-[1-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-4-phenylmethoxyindol-3-yl]-2-phenylacetic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0025	uM
3-[4-[(N-pentanoylanilino)methyl]phenyl]benzoic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0025	uM
4-[4-[(N-pentanoylanilino)methyl]phenyl]benzoic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0025	uM
N-phenyl-N-[[4-[4-(4-propan-2-ylpiperazine-1-carbonyl)phenyl]phenyl]methyl]pentanamide	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0026	uM
3-[4-[4-[(3-fluoro-N-pentanoylanilino)methyl]phenyl]phenoxy]propanoic acid	2142892: Antagonist activity at human BLT2 expressed in CHO cells assessed as inhibition of LTB4 induced cell migration measured after 3 hrs by chemotaxis assay	ic50	0.0027	uM
2-[3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-2-propylphenoxy]-4-fluorobenzoic acid	91333: Inhibition of LTB4 induced expression of human neutrophil integrin CD11b/CD18.	ic50	0.0027	uM
4-ethyl-2-(4-fluorophenyl)-5-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenol	102636: Binding affinity towards human LTB4 receptor measured as inhibition of binding of [3H]LTB4 to isolated human neutrophils	ki	0.0028	uM
7-[3-(2-ethyl-5-hydroxy-4-phenylphenoxy)propoxy]-8-propyl-3,4-dihydro-2H-chromene-2-carboxylic acid	102297: Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand	ki	0.0028	uM
5-[4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalen-2-yl]pentanoic acid	102287: LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane	ic50	0.0028	uM
2-[[3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]-2-propylphenyl]methyl]benzoic acid	91333: Inhibition of LTB4 induced expression of human neutrophil integrin CD11b/CD18.	ic50	0.0028	uM
sodium 4-ethyl-2-(4-fluorophenyl)-5-[6-methyl-6-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)heptoxy]phenol	90989: Inhibition of [3H]LTB4 receptor binding in human neutrophils	ic50	0.0028	uM
4-ethyl-2-(4-methoxyphenyl)-5-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenol	102636: Binding affinity towards human LTB4 receptor measured as inhibition of binding of [3H]LTB4 to isolated human neutrophils	ki	0.0029	uM
sodium 4-ethyl-2-(4-methoxyphenyl)-5-[6-methyl-6-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)heptoxy]phenol	90989: Inhibition of [3H]LTB4 receptor binding in human neutrophils	ic50	0.0029	uM
sodium 4-ethyl-5-[6-methyl-6-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)heptoxy]-2-phenylphenol	90989: Inhibition of [3H]LTB4 receptor binding in human neutrophils	ic50	0.0030	uM
sodium 4-ethyl-2-(3-fluorophenyl)-5-[6-methyl-6-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)heptoxy]phenol	90989: Inhibition of [3H]LTB4 receptor binding in human neutrophils	ic50	0.0030	uM

CTD chemical–gene interactions

19 total (human), top 19 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression	2
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
mancozeb	increases expression	1
2,4,5,2’,4’,5’-hexachlorobiphenyl	decreases expression	1
3,4,5,3’,4’-pentachlorobiphenyl	decreases expression	1
perfluorooctanoic acid	decreases expression	1
5,12,20-trihydroxy-6,8,10,14-eicosatetraenoic acid	affects binding	1
leukotriene B5	affects binding	1
di-n-butylphosphoric acid	affects expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Arachidonic Acids	affects binding	1
Benzo(a)pyrene	decreases methylation	1
Hydroxyeicosatetraenoic Acids	affects binding	1
Leukotriene B4	affects binding	1
Plant Extracts	affects cotreatment, decreases expression	1
Smoke	decreases expression	1
Tobacco Smoke Pollution	decreases expression	1

ChEMBL screening assays

81 unique, capped per target: 48 binding, 33 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3268220	Binding	Binding affinity to leukotriene B4 receptor (unknown origin)	Cathepsin C inhibitors: property optimization and identification of a clinical candidate. — J Med Chem
CHEMBL683518	Functional	Inhibition of LTB4 induced bronchospasm in guinea pig was determined in at 50 mg/kg i.d.	Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters. — J Med Chem

Cellosaurus cell lines

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

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

Cellosaurus	Name	Category	Sex
CVCL_B1W8	Abcam HeLa LTB4R2 KO	Cancer cell line	Female
CVCL_T764	CHO-HA-hBLT2	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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