LTB4R

Summary

LTB4R (leukotriene B4 receptor, HGNC:6713) is a protein-coding gene on chromosome 14q12, encoding Leukotriene B4 receptor 1 (Q15722). Receptor for extracellular ATP > UTP and ADP.

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 signal transduction. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 1241 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 62 total
• Druggable target: yes — 7 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001143919

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6713
Approved symbol	LTB4R
Name	leukotriene B4 receptor
Location	14q12
Locus type	gene with protein product
Status	Approved
Aliases	BLTR, P2Y7, LTB4R1
Ensembl gene	ENSG00000213903
Ensembl biotype	protein_coding
OMIM	601531
Entrez	1241

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 13 protein_coding

ENST00000345363, ENST00000396782, ENST00000396789, ENST00000553481, ENST00000556141, ENST00000862011, ENST00000862012, ENST00000862013, ENST00000924166, ENST00000924167, ENST00000924168, ENST00000960477, ENST00000960478

RefSeq mRNA: 2 — MANE Select: NM_001143919 NM_001143919, NM_181657

CCDS: CCDS9626

Canonical transcript exons

ENST00000345363 — 2 exons

Exon	Start	End
ENSE00001492671	24311502	24311804
ENSE00001526241	24315637	24318036

Expression profiles

Bgee: expression breadth ubiquitous, 133 present calls, max score 97.53.

FANTOM5 (CAGE): breadth broad, TPM avg 1.4520 / max 237.9970, expressed in 339 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139031	1.2996	303
139032	0.1267	68
139033	0.0157	4
139034	0.0100	4

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	97.53	gold quality
skin of abdomen	UBERON:0001416	95.94	gold quality
esophagus mucosa	UBERON:0002469	95.84	gold quality
zone of skin	UBERON:0000014	95.61	gold quality
blood	UBERON:0000178	95.45	gold quality
skin of leg	UBERON:0001511	95.41	gold quality
monocyte	CL:0000576	93.15	gold quality
leukocyte	CL:0000738	92.96	gold quality
granulocyte	CL:0000094	92.38	gold quality
spleen	UBERON:0002106	90.45	gold quality
vagina	UBERON:0000996	89.80	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	89.49	gold quality
bone marrow	UBERON:0002371	87.30	gold quality
minor salivary gland	UBERON:0001830	85.96	gold quality
bone marrow cell	CL:0002092	85.92	gold quality
esophagus	UBERON:0001043	85.57	gold quality
right uterine tube	UBERON:0001302	85.47	gold quality
saliva-secreting gland	UBERON:0001044	84.57	gold quality
right lobe of liver	UBERON:0001114	83.89	gold quality
ectocervix	UBERON:0012249	83.52	gold quality
right lung	UBERON:0002167	82.62	gold quality
subcutaneous adipose tissue	UBERON:0002190	81.55	gold quality
uterine cervix	UBERON:0000002	81.52	gold quality
adipose tissue	UBERON:0001013	81.28	gold quality
omental fat pad	UBERON:0010414	81.09	gold quality
upper lobe of left lung	UBERON:0008952	81.06	gold quality
left adrenal gland cortex	UBERON:0035825	80.84	gold quality
prostate gland	UBERON:0002367	80.83	gold quality
vermiform appendix	UBERON:0001154	80.43	gold quality
small intestine Peyer’s patch	UBERON:0003454	80.39	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ENAD-17	no	3.11
E-ANND-3	no	2.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): NFE2L2, RUNX1

miRNA regulators (miRDB)

45 targeting LTB4R, 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-4455	100.00	65.48	1587
HSA-MIR-6844	99.82	70.69	2423
HSA-MIR-4639-5P	99.81	67.37	1028
HSA-MIR-6892-3P	99.68	66.40	1178
HSA-MIR-12124	99.68	69.17	2700
HSA-MIR-5004-5P	99.68	66.63	1294
HSA-MIR-3158-5P	99.65	67.51	1763
HSA-MIR-7150	99.62	66.80	1322
HSA-MIR-24-3P	99.59	69.97	1934
HSA-MIR-4328	99.57	71.06	4094
HSA-MIR-141-5P	99.57	67.86	897
HSA-MIR-642A-5P	99.51	65.10	1152
HSA-MIR-133A-5P	99.28	69.13	941
HSA-MIR-3922-3P	99.25	64.96	1136
HSA-MIR-3176	99.25	64.35	954
HSA-MIR-149-5P	99.25	67.16	1315
HSA-MIR-4727-5P	99.23	67.55	1154
HSA-MIR-6744-3P	99.22	64.41	972
HSA-MIR-4757-5P	99.12	64.51	981
HSA-MIR-877-3P	99.09	68.10	1637
HSA-MIR-4752	98.71	68.04	833
HSA-MIR-1237-3P	98.55	67.65	1423
HSA-MIR-376B-5P	98.46	66.40	606
HSA-MIR-376C-5P	98.46	66.64	589
HSA-MIR-499B-5P	98.35	68.39	988
HSA-MIR-1304-3P	98.29	66.44	1207
HSA-MIR-561-5P	98.25	68.13	1365
HSA-MIR-615-5P	98.10	63.76	591
HSA-MIR-744-3P	97.99	67.76	637
HSA-MIR-4294	97.86	65.72	1110

Literature-anchored findings (GeneRIF, showing 40)

• Up-regulation of leukotriene B4 receptor-1 expression by the glucocorticoid dexamethasone provides a mechanism for enhanced LTB4-induced neutrophil survival. (PMID:11907121)
• marked expression of leukotriene B(4) receptor in human pancreatic cancer tissues (PMID:12163367)
• Results show that leukotriene B(4) binds BLT1 and activates G(i)-like protein, and both phosphatidylinositol 3-kinase (PI3-K) activation and a sustained calcium elevation by calcium influx are necessary for enzyme release in these cells. (PMID:12244116)
• an examination of in vivo chemotaxis using CHO cells expressing this receptor (PMID:12664610)
• BLT1 is a high-affinity receptor specific for leukotriene B4 on leukocytes; the 352 amino acid sequence is 78% identical to the mouse receptor (PMID:12895595)
• helix 8 of LTB4 receptor 1 plays an important role in the conformational change of the receptor to the low affinity state after G-protein activation, possibly by sensing the status of coupling Galpha subunits as GTP-bound (PMID:12902330)
• 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)
• Glucocorticoids up-regulate leukotriene B4 receptor-1 expression during neutrophilic differentiation of HL-60 cells (PMID:12943671)
• LTB4R has dileucine motifs and an alpha-helix VIII which regulate its expression (PMID:14688279)
• BLT1 expression in human monocytes is regulated by pro- and anti-inflammatory cytokines, lipopolysaccharide (LPS), and dexamethasone. (PMID:15728714)
• LTB4 production and subsequent activation of the high affinity LTB4 receptor in calcium mobilization of neutrophils. (PMID:15789613)
• essential role for BLT1 in allergen-mediated CD8+ T cell recruitment into the lung and development of airway hyperresponsiveness and inflammation (PMID:15814727)
• LTB(4) activates functional BLT(1) receptors on vascular smooth muscle cells, inducing chemotaxis and proliferation, and that BLT(1) receptors were up-regulated through an Ikappa kinase beta/NF-kappaB-dependent pathway. (PMID:16293697)
• A role for BLT1 is defined using transgenic BLT1-deficient effector CD8-positive T cells that mediate increased airway reactivity when transferred into CD8-deficient mice (PMID:16493075)
• 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)
• This review summarizes the role of the LTB4/BLT1 pathway, an impotant target for the treatment of bronchial asthma. (PMID:17075244)
• The conformational changes in each subunit of a receptor dimer resulting from agonist binding to either one or both subunits by measuring the fluorescent properties of a leukotriene B(4) receptor dimer, was analyzed. (PMID:17139258)
• The extended cytoplasmic helix connected to transmembrane helix V of BLT1 might be a key region for selective activation of the GTP-binding protein Gi alpha subunit. (PMID:17158791)
• The ligand binding site and activation mechanism for BLT1 have been characterized. (PMID:17237498)
• A new class of phospholipid-like surfactants that stabilize the G protein-coupled receptor, BLT1. (PMID:17445804)
• stimulation of neutrophils with LTB(4) (in the presence or absence of CMV) leads to the release of myeloperoxidase, alpha-defensins, eosinophil-derived neurotoxin, and the human cathelicidin LL-37 in a BLT1-dependent manner. (PMID:17931111)
• Genetic variation in leukotriene pathway members and their receptors confer an increased risk of ischemic stroke in 2 independent populations (PMID:18323512)
• BLT1 was expressed in 34% of ovarian neoplasms. (PMID:18421027)
• Report the long-term effect of Helicobacter pylori eradication on COX-1/2, 5-LOX and leukotriene receptors in patients with a risk gastritis phenotype–a link to gastric carcinogenesis. (PMID:18571838)
• increased expression in allergic diseases (PMID:18797182)
• 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)
• neutrophil-chemotactic activity of the conditioned media from the intraluminal thrombus exhibited major inhibition by antagonists of the leukotriene B(4) receptors (PMID:19136615)
• Introduction of a metal-binding site connecting the third and sixth transmembrane domains of the BLT1 receptor stabilizes its ground state. (PMID:19309698)
• AML1 enhances BLT1 expression by binding to AE-BLex, which is accessible in leukocytes. (PMID:20395453)
• Leukotriene B(4) BLT receptor signaling regulates the level and stability of cyclooxygenase-2 (COX-2) mRNA through restricted activation of Ras/Raf/ERK/p42 AUF1 pathway (PMID:20489206)
• Upon stimulation with LTB(4) or LPS, more BLT(1) protein is found on HUVEC cells, now evenly distributed over the cytoplasm and in the cell nucleus, but less on the cell surface (PMID:20688055)
• leukotriene B(4) receptors (BLT(1) and BLT(2)) are differently expressed in fibroblast from peripheral versus central airways in asthmatics and healthy controls. (PMID:21596548)
• The polymorphisms spanning LTB4R is not major determinants of baseline lung function in smokers. (PMID:22206291)
• 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)
• Helix 8 of BLT1 inhibits receptor internalization by suppressing the excessive phosphorylation of the C-terminal tail. (PMID:22707565)
• The LTB(4)-BLT signaling pathway may negatively regulate preadipocyte differentiation via induction of TGFBI expression as a rate-limiting system to control adipocyte differentiation. (PMID:23137534)
• LTB4R1 shows splice variation in the 5’-untranslated region and multiple promoter regions. LTB4R1 polymorphisms do not appear to be susceptibility markers for the development of asthma in Caucasian subjects. (PMID:23167751)
• A novel method predicts activated structures of G-protein-coupled receptor BLT1 with high accuracy, while aiming for the use of the predicted 3D structures in in silico virtual screening. (PMID:23304088)
• we show that orchestrated action of CXCR2 and leukotriene B4 receptor BLT1 plays a key role in neutrophil recruitment during the development of imiquimod (IMQ)-induced psoriatic skin lesions in mice (PMID:24663678)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ltb4r	ENSDARG00000032631
rattus_norvegicus	Ltb4r	ENSRNOG00000080793
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), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Leukotriene B4 receptor 1 — Q15722 (reviewed: Q15722)

Alternative names: Chemoattractant receptor-like 1, G-protein coupled receptor 16, P2Y purinoceptor 7

All UniProt accessions (3): G3V244, G3V4Q5, Q15722

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for extracellular ATP > UTP and ADP. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. May be the cardiac P2Y receptor involved in the regulation of cardiac muscle contraction through modulation of L-type calcium currents. Is a receptor for leukotriene B4, a potent chemoattractant involved in inflammation and immune response.

Subcellular location. Cell membrane.

Tissue specificity. Expressed at highest levels in heart, skeletal muscle and at lower levels in brain and liver. High level of expression in lymphoid tissues.

Post-translational modifications. Phosphorylated by GRK6 upon leukotriene B4 binding; which promotes desensitization.

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

RefSeq proteins (2): NP_001137391, NP_858043 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000826	Formyl_rcpt-rel	Family
IPR003981	Leukotriene_B4_rcpt	Family
IPR003983	Leukotriene_B4_typ-1_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (45 total): helix 14, topological domain 8, transmembrane region 7, strand 4, sequence conflict 3, compositionally biased region 2, glycosylation site 2, mutagenesis site 2, chain 1, region of interest 1, sequence variant 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
7K15	X-RAY DIFFRACTION	2.88
7VKT	ELECTRON MICROSCOPY	2.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q15722-F1	81.93	0.47

Antibody-complex structures (SAbDab): 1 — 7VKT

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 (2): 2, 164

Mutagenesis-validated functional residues (2):

Position	Phenotype
308	no effect on affinity for leukotriene b4, induces resistance to desensitization by grk6, but minor effect on phosphoryla
310	no effect on affinity for leukotriene b4 or on desensitization by grk6.

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: 138 (showing top): GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, JAEGER_METASTASIS_DN, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, DARWICHE_SKIN_TUMOR_PROMOTER_UP, DARWICHE_PAPILLOMA_RISK_LOW_UP, DARWICHE_PAPILLOMA_RISK_HIGH_UP, DARWICHE_SQUAMOUS_CELL_CARCINOMA_DN, chr14q12, RICKMAN_TUMOR_DIFFERENTIATED_WELL_VS_POORLY_DN, GOBP_MUSCLE_CONTRACTION, RUTELLA_RESPONSE_TO_HGF_VS_CSF2RB_AND_IL4_DN, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, SANSOM_APC_TARGETS_DN, PU1_Q6

GO Biological Process (8): muscle contraction (GO:0006936), inflammatory response (GO:0006954), immune response (GO:0006955), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), neuropeptide signaling pathway (GO:0007218), signal transduction (GO:0007165), leukotriene signaling pathway (GO:0061737)

GO Molecular Function (5): nucleotide binding (GO:0000166), 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 (2): 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	4
G protein-coupled receptor activity	2
muscle system process	1
defense response	1
immune system process	1
response to stimulus	1
signal transduction	1
phospholipase C activator activity	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
leukotriene receptor activity	1
icosanoid receptor activity	1
leukotriene signaling pathway	1
peptide receptor activity	1
transmembrane signaling receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

978 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LTB4R	LTA4H	P09960	843
LTB4R	RARRES2	Q99969	841
LTB4R	HSH2D	Q96JZ2	726
LTB4R	CXCL8	P10145	721
LTB4R	ALOX5	P09917	720
LTB4R	ALOX5AP	P20292	647
LTB4R	LTC4S	Q16873	634
LTB4R	PTGER3	P43115	623
LTB4R	CXCL1	P09341	612
LTB4R	CD4	P01730	604
LTB4R	CMKLR1	Q99788	604
LTB4R	GRK6	P43250	532
LTB4R	GPR32	O75388	531
LTB4R	LTB4R2	Q9NPC1	529
LTB4R	CDR2	Q01850	527

IntAct

3 interactions, top by confidence:

A	B	Type	Score
LTB4R	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
LTB4R	YWHAG	psi-mi:“MI:0915”(physical association)	0.370

BioGRID (17): CYBB (Affinity Capture-Western), LTB4R (Negative Genetic), PIK3CG (Negative Genetic), LTB4R (Negative Genetic), MAP2K5 (Positive Genetic), NR5A1 (Positive Genetic), LTB4R (Affinity Capture-RNA), LTB4R (Affinity Capture-RNA), YWHAG (Two-hybrid), LTB4R (Reconstituted Complex), LTB4R (Reconstituted Complex), LTB4R (Reconstituted Complex), LTB4R (FRET), LTB4R (Reconstituted Complex), LTB4R (FRET)

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: A0A287A2K5, C8YUV0, O00155, O02836, O08786, O15973, O18935, O19012, O19014, O19025, O19032, O19054, O19091, O62729, O77408, O77700, O77721, O77830, O97665, O97772, P04761, P08482, P0C5I1, P11229, P12657, P17200, P18089, P19328, P22270, P25021, P30545, P30551, P30552, P30553, P30796, P32211, P32238, P32239, P32302, P46627

SIGNOR signaling

7 interactions.

A	Effect	B	Mechanism
LTB4R	“up-regulates activity”	GNAI1	binding
LTB4R	“up-regulates activity”	GNAI3	binding
LTB4R	“up-regulates activity”	GNAO1	binding
LTB4R	“up-regulates activity”	GNA14	binding
LTB4R	“up-regulates activity”	GNA12	binding
“leukotriene B4(1-)”	“up-regulates activity”	LTB4R	“chemical activation”
GRK6	“down-regulates activity”	LTB4R	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	53
Likely benign	4
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

406 predictions. Top by Δscore:

Variant	Effect	Δscore
14:24311628:G:T	donor_gain	1.0000
14:24311600:G:T	donor_gain	0.9900
14:24311601:G:GT	donor_gain	0.9900
14:24311601:G:T	donor_gain	0.9900
14:24311628:G:GT	donor_gain	0.9900
14:24311664:A:T	donor_gain	0.9900
14:24311593:GCTC:G	donor_gain	0.9800
14:24311600:G:GT	donor_gain	0.9800
14:24311661:C:G	donor_gain	0.9800
14:24315884:T:TA	acceptor_gain	0.9800
14:24311667:GTG:G	donor_gain	0.9700
14:24311669:G:GA	donor_gain	0.9600
14:24311629:A:T	donor_gain	0.9400
14:24311668:T:TA	donor_gain	0.9400
14:24315631:CTCCA:C	acceptor_loss	0.9400
14:24315632:TCCA:T	acceptor_loss	0.9400
14:24315633:CCAG:C	acceptor_loss	0.9400
14:24315634:CAGGT:C	acceptor_loss	0.9400
14:24315635:AGGT:A	acceptor_loss	0.9400
14:24315636:G:GC	acceptor_loss	0.9400
14:24311589:G:GT	donor_gain	0.9300
14:24311633:G:T	donor_gain	0.9300
14:24311560:C:T	donor_gain	0.8900
14:24313904:G:T	acceptor_gain	0.8900
14:24315789:G:GT	donor_gain	0.8900
14:24311611:G:GT	donor_gain	0.8800
14:24313896:A:T	acceptor_gain	0.8700
14:24315635:A:AG	acceptor_gain	0.8600
14:24315636:G:GG	acceptor_gain	0.8600
14:24314870:T:TA	acceptor_gain	0.8500

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000251068 (14:24314478 C>T), RS1000657788 (14:24313263 G>A), RS1001512399 (14:24310053 C>T), RS1001777583 (14:24312013 T>A,C), RS1002362910 (14:24317153 A>G), RS1002460917 (14:24314013 A>C,T), RS1002566053 (14:24313250 C>T), RS1002673535 (14:24317079 CAT>C), RS1002782766 (14:24313691 T>G), RS1004288668 (14:24310888 C>T), RS1004914440 (14:24314986 A>G), RS1005027728 (14:24309682 T>A), RS1005807057 (14:24318222 T>A), RS1006376664 (14:24312431 G>A,C), RS1007632936 (14:24313151 G>A,C)

Disease associations

OMIM: gene MIM:601531 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST002371_1	Parent of origin effect on language impairment (paternal)	4.000000e-08

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2095160 (PROTEIN FAMILY), CHEMBL3911 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

7 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 23,586 (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
CHEMBL93	ZILEUTON	4	21,372
CHEMBL22016	ABLUKAST	2	1,780
CHEMBL301829	CP-195543	2	83
CHEMBL329123	ETALOCIB	2	154
CHEMBL89326	MOXILUBANT	2	23
CHEMBL90214	TICOLUBANT	2	136
CHEMBL3286797	PF-04418948	1	38

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 (16 total), top 16:

Ligand	Action	Affinity	Parameter
[3H]LTB4	Full agonist	9.8	pKd
LTB4	Full agonist	9.4	pKi
BIIL 260	Antagonist	8.54	pIC50
CP-195543	Antagonist	8.17	pKi
CP105696	Antagonist	8.1	pIC50
20-hydroxy-LTB4	Full agonist	8.1	pKi
RO5101576	Antagonist	8.1	pIC50
[3H]CGS23131	Antagonist	7.9	pKd
etalocib	Antagonist	7.75	pKi
12R-HETE	Full agonist	7.5	pKi
VI-8	Antagonist	6.92	pKd
LY255283	Antagonist	6.6	pKi
BF-2	Antagonist	6.59	pIC50
U75302	Antagonist	6.4	pKi
ONO-4057	Antagonist	6.15	pIC50
SC-41930	Antagonist	6.1	pIC50

Binding affinities (BindingDB)

71 measured of 81 human assays (84 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
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
N-(tert-Butylsulfonyl)-4-fluoro-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	2 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
NSC_5311297	KI	2.3 nM
2-[(3R,4R)-4-hydroxy-3-[(2-phenyl-1,3-oxazol-4-yl)methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	3 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
NSC_5283125	KI	3.7 nM
4-Fluoro-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-((1-methylcyclopropyl)sulfonyl)benzamide	EC50	4 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(Cyclopropylsulfonyl)-4-fluoro-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	4 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((3S,4R or 3R,4S)-4-hydroxy-3-((2-phenyloxazol-4-yl)methyl)chroman-7-yl)benzamide	EC50	5 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-tert-butylsulfonyl-2-[(3R,4S)-4-hydroxy-3-[[5-(1,3-thiazol-5-yl)-2-pyridinyl]methyl]-3,4-dihydro-2H-chromen-7-yl]benzamide	EC50	5 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((rac-trans)-4-hydroxy-3-((5-(2-methylthiazol-5-yl)pyridin-2-yl)methyl)chroman-7-yl)benzamide	EC50	5 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
LTB4-3-aminopropylamide	KI	5.1 nM
4-Fluoro-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-((trifluoromethyl)sulfonyl)benzamide	EC50	6 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(3R,4S)-4-hydroxy-3-[[5-(1,3-thiazol-5-yl)-2-pyridinyl]methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	6 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
2-[(3S,4R)-4-hydroxy-3-[[5-(1,3-thiazol-5-yl)-2-pyridinyl]methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	6 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
N-(Cyclopropylsulfonyl)-2-((rac-trans)-4-hydroxy-3-((5-(2-methylthiazol-5-yl)pyridin-2-yl)methyl)chroman-7-yl)benzamide	EC50	6 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((rac-trans)-4-hydroxy-3-((5-(thiazol-5-yl)pyridin-2-yl)methyl)chroman-7-yl)benzamide	EC50	8 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
N-tert-butylsulfonyl-2-[(3S,4R)-4-hydroxy-3-(1,3-thiazol-4-ylmethyl)-3,4-dihydro-2H-chromen-7-yl]benzamide	EC50	11 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-((Rac-trans)-3-([1,1′-Biphenyl]-4-ylmethyl)-4-hydroxychroman-7-yl)-4-fluoro-N-((trifluoromethyl)sulfonyl)benzamide	EC50	11 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(Cyclopropylsulfonyl)-2-((rac-trans)-4-hydroxy-3-((5-(thiazol-5-yl)pyridin-2-yl)methyl)chroman-7-yl)benzamide	EC50	12 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
2-((3S,4R or 3R,4S)-3-Benzyl-4-hydroxychroman-7-yl)-N-((1-methylcyclopropyl)sulfonyl)benzamide	EC50	15 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-(Rac-trans)-4-Hydroxy-3-((2-phenyloxazol-4-yl)methyl)chroman-7-yl)-N-((1-methylcyclopropyl)sulfonyl)benzamide	EC50	15 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(3S,4R)-4-hydroxy-3-(1,3-thiazol-4-ylmethyl)-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	16 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	17 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-((3S,4R or 3R,4S)-3-Benzyl-4-hydroxychroman-7-yl)-N-(cyclopropylsulfonyl)benzamide	EC50	17 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(3S,4R)-4-hydroxy-3-[(2-phenyl-1,3-oxazol-4-yl)methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	19 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
LTB4-20-carboxy	KI	20 nM
2-((3S,4R or 3R,4S)-4-Hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-((1-methylcyclopropyl)sulfonyl)benzamide	EC50	22 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-((Cyclopropylmethyl)sulfonyl)-2-((3,4-trans)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	23 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-((3,4-trans)-4-Hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-(isobutylsulfonyl)benzamide	EC50	24 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
(5R)-6-[6-[(1E,3S,5Z)-3-hydroxyundeca-1,5-dienyl]pyridin-2-yl]hexane-1,5-diol	KI	25 nM
2-[(3R,4R)-4-hydroxy-3-(1,3-thiazol-4-ylmethyl)-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	26 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
LTB4-14,15-dehydro	KI	27 nM
N-(Cyclopropylsulfonyl)-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	28 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
4-fluoro-2-[(3S,4R)-4-hydroxy-3-[(4-phenylphenyl)methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(trifluoromethylsulfonyl)benzamide	EC50	35 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-tert-butylsulfonyl-2-[(3S,4R)-3-[(2-ethylpyrazol-3-yl)methyl]-4-hydroxy-3,4-dihydro-2H-chromen-7-yl]benzamide	EC50	36 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-((Rac-cis)-3-([1,1′-Biphenyl]-4-ylmethyl)-4-hydroxychroman-7-yl)-4-fluoro-N-((trifluoromethyl)sulfonyl)benzamide	EC50	37 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-((3,4-trans)-4-Hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-(neopentylsulfonyl)benzamide	EC50	44 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(Cyclopentylsulfonyl)-2-((3,4-trans)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	48 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(3R,4S)-4-hydroxy-3-[(2-phenyl-1,3-oxazol-4-yl)methyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	60 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(4S)-4-hydroxy-3-[(1S)-1-pyridin-2-ylethyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	67 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
4-Fluoro-2-((3S,4R or 3R,4S)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)-N-(methylsulfonyl)benzamide	EC50	93 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((rac-trans)-4-hydroxy-3-((1-methyl-1H-pyrazol-5-yl)methyl)chroman-7-yl)benzamide	EC50	95 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-tert-butylsulfonyl-2-[(3S,4R)-4-hydroxy-3-[[5-(1,3-thiazol-5-yl)-2-pyridinyl]methyl]-3,4-dihydro-2H-chromen-7-yl]benzamide	EC50	128 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists
N-(tert-Butylsulfonyl)-2-((3R,4S or 3S,4R)-4-hydroxy-3-(pyridin-2-ylmethyl)chroman-7-yl)benzamide	EC50	144 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
2-[(4S)-4-hydroxy-3-[(1R)-1-pyridin-2-ylethyl]-3,4-dihydro-2H-chromen-7-yl]-N-(1-methylcyclopropyl)sulfonylbenzamide	EC50	154 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
LTB4-6-trans	KI	336 nM
2-(Rac-trans)-4-Hydroxy-3-((1-methyl-1H-pyrazol-5-yl)methyl)chroman-7-yl)-N-((1-methylcyclopropyl)sulfonyl)benzamide	EC50	360 nM	US-10336733: Aryl acylsulfonamides as BLT1 antagonists
N-(Cyclopropylsulfonyl)-2-((3R,4S or 3S,4R)-4-hydroxy-3-((5-(2-methylthiazol-5-yl)pyridin-2-yl)methyl)chroman-7-yl)benzamide	EC50	391 nM	US-10370368: Aryl acylsulfonamides as BLT1 antagonists

ChEMBL bioactivities

1167 potent at pChembl≥5 of 1210 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
10.15	IC50	0.07	nM	CHEMBL1099326
10.14	Ki	0.073	nM	CHEMBL62265
10.00	IC50	0.1	nM	CHEMBL422388
9.96	Ki	0.11	nM	CHEMBL340460
9.92	Ki	0.12	nM	LEUKOTRIENE_B4
9.85	Ki	0.14	nM	CHEMBL262231
9.85	Ki	0.14	nM	CHEMBL328712
9.82	IC50	0.15	nM	CHEMBL167350
9.74	IC50	0.18	nM	CHEMBL1099335
9.70	IC50	0.2	nM	CHEMBL1099332
9.68	IC50	0.21	nM	CHEMBL1099323
9.66	IC50	0.22	nM	CHEMBL1094346
9.44	IC50	0.36	nM	CHEMBL1099331
9.44	IC50	0.36	nM	CHEMBL328712
9.42	IC50	0.38	nM	CHEMBL1094347
9.41	IC50	0.39	nM	CHEMBL1099334
9.36	IC50	0.44	nM	CHEMBL1098560
9.35	IC50	0.45	nM	CHEMBL125723
9.33	Ki	0.47	nM	CHEMBL292782
9.32	IC50	0.48	nM	CHEMBL1099330
9.24	Ki	0.57	nM	CHEMBL340460
9.24	IC50	0.57	nM	CHEMBL1099333
9.24	IC50	0.58	nM	CHEMBL1098550
9.24	IC50	0.58	nM	CHEMBL1099337
9.24	IC50	0.58	nM	CHEMBL125646
9.22	IC50	0.6	nM	CHEMBL126200
9.21	IC50	0.61	nM	CHEMBL1094349
9.15	Ki	0.71	nM	CHEMBL136700
9.11	Ki	0.78	nM	TICOLUBANT
9.10	Ki	0.8	nM	TICOLUBANT
9.10	IC50	0.8	nM	CHEMBL125214
9.10	IC50	0.8	nM	CHEMBL328712
9.07	IC50	0.85	nM	CHEMBL167804
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	IC50	1	nM	SC-41390
9.00	Ki	1	nM	CHEMBL112520
9.00	Ki	1	nM	CHEMBL5428366
9.00	Ki	1	nM	CHEMBL95453
9.00	IC50	1	nM	CHEMBL125559
9.00	IC50	1	nM	CHEMBL333493
9.00	Ki	1	nM	CHEMBL112487
9.00	IC50	1	nM	CHEMBL341116
9.00	IC50	1	nM	CHEMBL137759
9.00	Ki	1	nM	CHEMBL98718
8.97	IC50	1.07	nM	CHEMBL123486
8.96	Ki	1.1	nM	CHEMBL62265

PubChem BioAssay actives

856 with measured affinity, of 1571 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
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalene-2-carboxylic acid	102305: Affinity for guinea pig PMN LTB-4 receptors.	ki	0.0001	uM
4-[2-(2-carboxyethyl)-3-[6-(3,5-dipyridin-4-ylphenoxy)hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	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-(2-carboxyethyl)-3-[6-[3-(3-fluorophenyl)-5-pyridin-4-ylphenoxy]hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0002	uM
4-[2-(2-carboxyethyl)-3-[6-(3-pyridin-4-yl-5-thiophen-3-ylphenoxy)hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0002	uM
4-[2-(2-carboxyethyl)-3-[6-(3,5-diphenylphenoxy)hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0002	uM
4-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-pyridin-4-ylphenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0002	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-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-thiophen-3-ylphenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0004	uM
4-[2-(2-carboxyethyl)-3-[6-(3-phenyl-5-thiophen-3-ylphenoxy)hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0004	uM
4-[2-(2-carboxyethyl)-3-[6-(3-pyrimidin-5-yl-5-thiophen-3-ylphenoxy)hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0004	uM
4-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-pyrimidin-5-ylphenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0004	uM
4-[2-(2-carboxyethyl)-3-[6-[(4,6-diphenyl-2-pyridinyl)oxy]hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0005	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
4-[2-(2-carboxyethyl)-3-[6-[3-(2-chloro-4-pyridinyl)-5-thiophen-3-ylphenoxy]hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0006	uM
4-[2-(2-carboxyethyl)-3-[6-[3,5-di(thiophen-3-yl)phenoxy]hexyl]phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0006	uM
4-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-phenylphenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	ic50	0.0006	uM
4-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-(2-fluorophenyl)phenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	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-[6-[(2,6-dichlorophenyl)sulfanylmethyl]-3-(2-phenylethoxy)-2-pyridinyl]prop-2-enoic acid	102637: Inhibition of [3H]LTB4 binding to human neutrophils	ki	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
3-[1-hydroxy-2-[6-[(E)-3-hydroxyundec-1-enyl]-2-pyridinyl]ethyl]benzoic acid	156045: Binding affinity of [3H]LTB4 to receptors on intact human polymorphonuclear leukocytes	ki	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
lithium 3-[1-hydroxy-2-[6-[(E)-3-hydroxyundec-1-enyl]-2-pyridinyl]ethyl]benzoate	102645: Inhibition of [3H]- LTB4 binding on human whole cells	ki	0.0010	uM
5-[2-(2-carboxyethyl)-3-[6-[(4-oxo-8-propyl-2,3-dihydrochromen-7-yl)oxy]hexyl]phenoxy]pentanoic acid	102635: Binding affinity at leukotriene B4 receptor on intact human PMNs by displacement of [3H]LTB4.	ki	0.0010	uM
6-[2-(2-carboxyethyl)-3-[6-[(4-oxo-8-propyl-2,3-dihydrochromen-7-yl)oxy]hexyl]phenoxy]hexanoic acid	102641: Compound was tested for inhibitory activity against human neutrophil LTB4 receptor binding	ki	0.0010	uM
6-[[4-(1,3-benzodioxol-5-yl)-6-phenyl-2-pyridinyl]oxy]hexanoic acid	102293: Inhibition of [3H]LTB4 binding to Leukotriene B4 receptor in the guinea pig spleen membranes.	ic50	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-[6-[(2,6-dichlorophenyl)sulfanylmethyl]-3-[2-(4-methoxyphenyl)ethoxy]-2-pyridinyl]prop-2-enoic acid	102637: Inhibition of [3H]LTB4 binding to human neutrophils	ki	0.0012	uM
4-[3-[6-[3-(1,3-benzodioxol-5-yl)-5-(3-fluorophenyl)phenoxy]hexyl]-2-(2-carboxyethyl)phenoxy]butanoic acid	482026: Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins	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
(E)-3-[3-[2-(4-chlorophenyl)ethoxy]-6-[(2,6-dichlorophenyl)sulfanylmethyl]-2-pyridinyl]prop-2-enoic acid	102637: Inhibition of [3H]LTB4 binding to human neutrophils	ki	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	102452: Compound was tested for inhibitory activity against human neutrophil LTB4 receptor binding	ic50	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
(E)-3-[6-[(2,6-dichlorophenyl)sulfanylmethyl]-3-(3-phenylpropoxy)-2-pyridinyl]prop-2-enoic acid	102637: Inhibition of [3H]LTB4 binding to human neutrophils	ki	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
(E)-3-[6-[(2,6-dichlorophenyl)sulfanylmethyl]-3-[2-(4-fluorophenyl)ethoxy]-2-pyridinyl]prop-2-enoic acid	102637: Inhibition of [3H]LTB4 binding to human neutrophils	ki	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-[7-[3-[2-(cyclopropylmethyl)-3-methoxy-4-(methylcarbamoyl)phenoxy]propoxy]-8-propyl-3,4-dihydro-2H-chromen-2-yl]propanoic acid	102452: Compound was tested for inhibitory activity against human neutrophil LTB4 receptor binding	ic50	0.0015	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
CP 105696	affects binding, decreases activity, decreases reaction	2
Tretinoin	affects expression, increases expression	2
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
potassium perchlorate	decreases expression	1
4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone	decreases expression	1
zinc chloride	decreases expression	1
tamibarotene	affects expression	1
LY 255283	affects binding, decreases activity, decreases reaction, increases activity	1
CGP 52608	affects binding, increases reaction	1
LY 293111	affects binding, decreases activity, decreases reaction, increases activity	1
abrine	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Allergens	affects cotreatment, increases expression	1
Vehicle Emissions	affects cotreatment, increases expression	1
Azacitidine	decreases expression	1
Benzo(a)pyrene	increases methylation	1
Calcitriol	decreases expression	1
Copper	affects binding, increases expression	1
Disulfiram	affects binding, increases expression	1
Formaldehyde	increases expression	1
Leukotriene B4	decreases reaction, affects binding, increases activity	1
Methotrexate	decreases expression	1
Nickel	increases expression	1
Quercetin	increases expression	1
Smoke	decreases expression	1
Tetrachlorodibenzodioxin	affects cotreatment, decreases expression	1
Tobacco Smoke Pollution	decreases expression	1
Triiodothyronine	affects cotreatment, decreases expression	1

ChEMBL screening assays

240 unique, capped per target: 166 binding, 73 functional, 1 admet

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
CHEMBL4810223	ADMET	Inhibition of LTB4 (unknown origin) at 0.1 to 1 uM	Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. — J Med Chem

Cellosaurus cell lines

6 cell lines: 5 spontaneously immortalized cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H453	CHO-K1/LTB4/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV44	cAMP Hunter CHO-K1 LTB4R Gi	Spontaneously immortalized cell line	Female
CVCL_KX91	PathHunter CHO-K1 LTB4R beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA66	PathHunter U2OS LTB4R Total GPCR Internalization	Cancer cell line	Female
CVCL_T763	CHO-FLAG-hBLT1	Spontaneously immortalized cell line	Female
CVCL_ZK72	GeneBLAzer LTB4R-Galpha15-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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