FPR3

Summary

FPR3 (formyl peptide receptor 3, HGNC:3828) is a protein-coding gene on chromosome 19q13.41, encoding N-formyl peptide receptor 3 (P25089). May function as a pattern recognition G-protein coupled receptor (PRR/GPCR) involved in innate recognition of peptides derived from a specific set of bacterial pathogens or host mitochondria as pathogen- and damage-associated molecular patterns (PAMPs and DAMPs).

Predicted to enable N-formyl peptide receptor activity and complement receptor activity. Predicted to be involved in several processes, including complement receptor mediated signaling pathway; phospholipase C-activating G protein-coupled receptor signaling pathway; and positive regulation of cytosolic calcium ion concentration. Predicted to act upstream of or within G protein-coupled receptor signaling pathway. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 2359 — RefSeq curated summary.

At a glance

• GWAS associations: 20
• Clinical variants (ClinVar): 39 total
• Druggable target: yes — 10 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002030

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3828
Approved symbol	FPR3
Name	formyl peptide receptor 3
Location	19q13.41
Locus type	gene with protein product
Status	Approved
Aliases	FPRH1, FMLPY, RMLP-R-I
Ensembl gene	ENSG00000187474
Ensembl biotype	protein_coding
OMIM	136539
Entrez	2359

Gene structure

Transcript identifiers

Ensembl transcripts: 5 — 5 protein_coding

ENST00000339223, ENST00000595991, ENST00000901092, ENST00000901093, ENST00000957103

RefSeq mRNA: 1 — MANE Select: NM_002030 NM_002030

CCDS: CCDS12841

Canonical transcript exons

ENST00000339223 — 2 exons

Exon	Start	End
ENSE00001379510	51823739	51826190
ENSE00001404479	51795157	51795331

Expression profiles

Bgee: expression breadth ubiquitous, 194 present calls, max score 87.17.

FANTOM5 (CAGE): breadth broad, TPM avg 6.1561 / max 293.8163, expressed in 319 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
177269	5.4744	312
177268	0.5914	143
177270	0.0903	53

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
gall bladder	UBERON:0002110	87.17	gold quality
rectum	UBERON:0001052	85.53	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	84.57	gold quality
amniotic fluid	UBERON:0000173	83.01	gold quality
right coronary artery	UBERON:0001625	82.94	gold quality
synovial joint	UBERON:0002217	82.46	gold quality
layer of synovial tissue	UBERON:0007616	82.37	gold quality
mucosa of sigmoid colon	UBERON:0004993	82.32	gold quality
vermiform appendix	UBERON:0001154	81.31	gold quality
calcaneal tendon	UBERON:0003701	77.56	gold quality
caecum	UBERON:0001153	77.49	gold quality
descending thoracic aorta	UBERON:0002345	77.49	gold quality
lymph node	UBERON:0000029	77.43	gold quality
upper lobe of left lung	UBERON:0008952	77.05	gold quality
upper lobe of lung	UBERON:0008948	76.85	gold quality
palpebral conjunctiva	UBERON:0001812	76.69	gold quality
left adrenal gland	UBERON:0001234	76.26	gold quality
left adrenal gland cortex	UBERON:0035825	75.82	gold quality
right adrenal gland cortex	UBERON:0035827	75.62	gold quality
lower lobe of lung	UBERON:0008949	75.46	gold quality
smooth muscle tissue	UBERON:0001135	75.30	gold quality
decidua	UBERON:0002450	75.21	gold quality
left coronary artery	UBERON:0001626	75.01	gold quality
colonic mucosa	UBERON:0000317	74.88	gold quality
right adrenal gland	UBERON:0001233	74.82	gold quality
germinal epithelium of ovary	UBERON:0001304	74.56	gold quality
omental fat pad	UBERON:0010414	74.56	gold quality
coronary artery	UBERON:0001621	74.50	gold quality
peritoneum	UBERON:0002358	74.50	gold quality
adrenal cortex	UBERON:0001235	74.48	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-MTAB-8410	yes	40.31
E-ANND-3	yes	18.91

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

65 targeting FPR3, 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-3646	100.00	73.56	5283
HSA-MIR-6759-5P	99.99	66.54	785
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-6755-5P	99.95	65.59	464
HSA-MIR-6772-5P	99.94	67.01	577
HSA-MIR-9718	99.94	68.91	918
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-374A-5P	99.90	71.34	2923
HSA-MIR-374B-5P	99.90	69.98	2734
HSA-MIR-95-5P	99.89	72.17	3973
HSA-MIR-548D-3P	99.87	70.67	4362
HSA-MIR-548BB-3P	99.86	70.58	4354
HSA-MIR-548AC	99.84	70.77	4351
HSA-MIR-548H-3P	99.84	70.80	4349
HSA-MIR-548Z	99.84	70.80	4349
HSA-MIR-4495	99.82	72.08	3080
HSA-MIR-4517	99.76	69.19	1867
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-7154-5P	99.69	70.52	1900
HSA-MIR-4470	99.66	69.35	1767
HSA-MIR-4804-3P	99.65	67.78	866
HSA-MIR-561-3P	99.64	70.90	3647
HSA-MIR-6757-3P	99.63	66.88	1089
HSA-MIR-217-5P	99.49	69.93	1419
HSA-MIR-12131	99.48	68.72	1673
HSA-MIR-766-5P	99.47	67.91	2225
HSA-MIR-20A-3P	99.44	69.10	1575
HSA-MIR-4735-5P	99.43	68.49	1780
HSA-MIR-548AV-3P	99.43	68.50	1721

Literature-anchored findings (GeneRIF, showing 20)

• Human dendritic cells express functional FPRL2 throughout maturation. FPRL2 & its endogenous ligand may be involved in regulating DC trafficking during Ag uptake & processing s well as the T-cell-stimulating phase of the immune responses. (PMID:12223529)
• investigated the direct effect of LXA4 as well as the effect on agonist-induced biological responses using transfected HL-60 cells expressing FPR, FPRL1 or FPRL2 (PMID:12410796)
• an annexin 1 peptide can activate FPR, FPRL1, and FPRL2; results indicate that annexin 1 participates in regulating leukocyte emigration into inflamed tissue by activating and desensitizing different receptors of the FPR family. (PMID:15187149)
• Results show that humanin (HN) acts as a ligand for formyl peptide receptor-like 1 (FPRL1) and 2 (FPRL2). (PMID:15465011)
• Activation of FPRL2 inhibits lipopolysaccharide-induced dendritic cell maturation. (PMID:16002663)
• However, F2L inhibits formyl peptide receptor (FPR) and FPRL1 activities, resulting in the inhibition of intracellular calcium increases, and superoxide generation induced by N-formyl-Met-Leu-Phe, MMK-1, or Trp-Lys-Tyr-Met-Val-d-Met in neutrophils. (PMID:17577578)
• FPRL2 is expressed and functional in macrophages differentiated from monocytes in vitro in different conditions (PMID:19342677)
• Human monocytes express FPR1, FPR2, and FPR3; human neutrophils express FPR1 and FPR2, but not FPR3. (PMID:19843937)
• Results show that uPAR expression regulates the adhesive and migratory ability of CXCR4-expressing cells through a mechanism involving fMLP receptors and alpha-v integrins. (PMID:20972812)
• N-formyl peptide receptor 3 (FPR3) departs from the homologous FPR2/ALX receptor with regard to the major processes governing chemoattractant receptor regulation, expression at the cell surface, and phosphorylation. (PMID:21543323)
• F2L peptide, derived from the processing of nanomolar concentrations of heme-binding protein (HEBP)1, is active on FPR3 and able to induce recruitment of FPR3-expressing monocytes, macrophages, and mouse neutrophils (PMID:21709160)
• transcriptional variations of FPR3 occur by an alternative promoter during primate evolution. (PMID:21717223)
• The demonstrated proper folding and functionality of the cell-free produced human FPR3 opens a new avenue for the fast and efficient generation of human FPRs (and even other GPCRs) for structural and functional analysis. (PMID:23746112)
• The H. pylori-derived peptide Hp(2-20) stimulated eosinophil migration through the engagement of FPR2 and FPR3, and also induced production of VEGF-A and TGF-beta, two key mediators of tissue remodelling. (PMID:24067461)
• Taken together, our results suggest that intracellular FPR in naive CD4 T cells and surface FPRs in activated CD4 T cells might regulate immune responses by regulating CD4 T cell activity. (PMID:29427663)
• These findings provide evidence for defective FPR2/3 and annexin A1 expressions that, associated with decreased M2a polarization, might be involved in the development of cigarette smoking induced persistent airflow limitation in chronic obstructive pulmonary disease. (PMID:29544524)
• Low FPR3 expression is associated with obstructive sleep apnea. (PMID:31116781)
• D-Peptide analogues of Boc-Phe-Leu-Phe-Leu-Phe-COOH induce neovascularization via endothelial N-formyl peptide receptor 3. (PMID:32152757)
• Formyl peptide receptor 2 is an emerging modulator of inflammation in the liver. (PMID:36750693)
• FPR3 reprograms glycolytic metabolism and stemness in gastric cancer via calcium-NFATc1 pathway. (PMID:38614385)

Cross-species orthologs

0 orthologs

Paralogs (8): C5AR2 (ENSG00000134830), GPR32 (ENSG00000142511), FPR2 (ENSG00000171049), FPR1 (ENSG00000171051), C3AR1 (ENSG00000171860), CMKLR1 (ENSG00000174600), C5AR1 (ENSG00000197405), GPR33 (ENSG00000214943)

Protein

Protein identifiers

N-formyl peptide receptor 3 — P25089 (reviewed: P25089)

Alternative names: FMLP-related receptor II, Formyl peptide receptor-like 2

All UniProt accessions (2): P25089, Q6L5J4

UniProt curated annotations — full annotation on UniProt →

Function. May function as a pattern recognition G-protein coupled receptor (PRR/GPCR) involved in innate recognition of peptides derived from a specific set of bacterial pathogens or host mitochondria as pathogen- and damage-associated molecular patterns (PAMPs and DAMPs). Low affinity receptor for a restricted repertoire of bacterial N-formylated peptides including fMKKIML from L. monocytogenes and fMPKLNR from V. cholerae. Contrary to FPR1 and FPR2 does not act as a receptor for fMLF peptide. High affinity receptor for N-acetylated F2L peptide derived from the cleavage of heme-binding protein HEBP1. F2L peptide binding may trigger chemotaxis of monocytes and dendritic cells to facilitate tissue repair. Low affinity receptor for N-acetylated Ac2-26 peptide derived from ANXA1, an anti-inflammatory and pro-resolving agonist. Ac2-26 peptide binding can direct myeloid cell chemotaxis within the inflammatory site where ANXA1 is at high concentrations, but it can also lead to receptor desensitization to limit the inflammatory response. Receptor for MT-RNR2/humanin, a mitochondrial-derived peptide that has an anti-inflammatory role in resolution of inflammation. Peptide binding leads to conformational changes coupled to heterotrimeric G(i) protein signaling. Upon GDP to GTP conversion, G(i)-alpha subunit dissociates from G-beta and G-gamma subunits. Free G(i)-alpha subunit inhibits cyclic adenylate cyclase and cAMP synthesis whereas the G-beta and G-gamma dimer activates downstream phospholipase C-beta and phosphoinositide 3-kinase signaling cascades leading to Ca(2+) influx.

Subunit / interactions. Heterodimer with FPR1.

Subcellular location. Cell membrane.

Tissue specificity. Detected in various tissues with highest expression in lung. Expressed in immature dendritic cells (at protein level).

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

RefSeq proteins (1): NP_002021* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000826	Formyl_rcpt-rel	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (24 total): topological domain 8, transmembrane region 7, sequence conflict 3, glycosylation site 2, chain 1, region of interest 1, compositionally biased region 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P25089-F1	83.62	0.58

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): 98–176

Glycosylation sites (2): 4, 10

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-418594	G alpha (i) signalling events
R-HSA-444473	Formyl peptide receptors bind formyl peptides and many other ligands

MSigDB gene sets: 146 (showing top): GOBP_INFLAMMATORY_RESPONSE, GOBP_TAXIS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_REGULATION_OF_IMMUNE_RESPONSE, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, MODULE_123, DODD_NASOPHARYNGEAL_CARCINOMA_UP, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, GOBP_PHOSPHOLIPASE_C_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, PID_UPA_UPAR_PATHWAY, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GOBP_ACTIVATION_OF_IMMUNE_RESPONSE, VERHAAK_GLIOBLASTOMA_MESENCHYMAL

GO Biological Process (9): complement receptor mediated signaling pathway (GO:0002430), chemotaxis (GO:0006935), inflammatory response (GO:0006954), signal transduction (GO:0007165), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), cell communication (GO:0007154), G protein-coupled receptor signaling pathway (GO:0007186), signaling (GO:0023052)

GO Molecular Function (4): complement receptor activity (GO:0004875), N-formyl peptide receptor activity (GO:0004982), G protein-coupled receptor activity (GO:0004930), 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
GPCR downstream signalling	1
Peptide ligand-binding receptors	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular process	2
G protein-coupled receptor signaling pathway	2
transmembrane signaling receptor activity	2
immune response-activating cell surface receptor signaling pathway	1
response to chemical	1
taxis	1
defense response	1
cell communication	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
phospholipase C activator activity	1
regulation of biological quality	1
G protein-coupled receptor activity	1
signal transduction	1
regulation of biological process	1
complement binding	1
complement receptor mediated signaling pathway	1
immune receptor activity	1
G protein-coupled peptide receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

936 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FPR3	HEBP1	Q9NRV9	946
FPR3	ANXA1	P04083	892
FPR3	CAMP	P49913	732
FPR3	PRNP	P04156	489
FPR3	VSTM2L	Q96N03	489
FPR3	GPR37	O15354	457
FPR3	CXCL8	P10145	457
FPR3	CXCL2	P19875	451
FPR3	CXCR2	P25025	450
FPR3	CCL19	Q99731	427
FPR3	CXCL14	O95715	426
FPR3	CCR1	P32246	422
FPR3	CXCL9	Q07325	422
FPR3	PLA2G7	Q13093	417
FPR3	FCER1G	P30273	416

IntAct

7 interactions, top by confidence:

A	B	Type	Score
RAMP1	FPR3	psi-mi:“MI:0915”(physical association)	0.400
FPR3	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
FPR3	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
FPR3	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	FPR3	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (4): FPR3 (Co-fractionation), FPR3 (Co-fractionation), FPR3 (Co-fractionation), FPR3 (Co-fractionation)

ESM2 similar proteins: A4FUQ5, B9VR26, O08790, O35786, O70129, O75388, O88416, O88536, O88537, O97664, P0C7U4, P21462, P21730, P25089, P25090, P30992, P30993, P33766, P35343, P35407, P46090, P46091, P79175, P79176, P79177, P79178, P79188, P79189, P79190, P79191, P79234, P79235, P79236, P79237, P79240, P79241, P79242, P79243, P97468, P97520

Diamond homologs: A4FUQ5, B1PHQ8, B9VR26, O08565, O08790, O35210, O35786, O62747, O70129, O75388, O77590, O88416, O88536, O88537, O97571, O97664, P0C7U4, P0C7U5, P21462, P21730, P25025, P25089, P25090, P25095, P25104, P28646, P29089, P29754, P29755, P30555, P30556, P30872, P30873, P30937, P30992, P30993, P31391, P33766, P34976, P35373

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
ANXA1	“up-regulates activity”	FPR3	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	29
Likely benign	7
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

366 predictions. Top by Δscore:

Variant	Effect	Δscore
19:51817762:T:TA	acceptor_gain	1.0000
19:51817766:A:AG	acceptor_gain	1.0000
19:51817767:A:G	acceptor_gain	1.0000
19:51795318:GATC:G	donor_gain	0.9900
19:51795329:GTG:G	donor_gain	0.9900
19:51795329:GTGGT:G	donor_loss	0.9900
19:51795331:GGTA:G	donor_loss	0.9900
19:51795332:GTA:G	donor_loss	0.9900
19:51795333:T:G	donor_loss	0.9900
19:51795332:G:GG	donor_gain	0.9800
19:51822852:A:AG	donor_gain	0.9800
19:51795328:GGTG:G	donor_gain	0.9700
19:51795329:GTGG:G	donor_gain	0.9700
19:51795330:TGGT:T	donor_gain	0.9700
19:51795331:G:GA	donor_gain	0.9700
19:51822797:G:GG	donor_gain	0.9700
19:51795327:TGGTG:T	donor_gain	0.9600
19:51795328:GGTGG:G	donor_gain	0.9600
19:51795330:TG:T	donor_gain	0.9400
19:51795331:GG:G	donor_gain	0.9400
19:51795334:AAG:A	donor_loss	0.9300
19:51822846:G:GT	donor_gain	0.9200
19:51822801:A:G	donor_gain	0.9100
19:51795313:A:T	donor_gain	0.8900
19:51817773:T:A	acceptor_gain	0.8900
19:51822796:A:G	donor_gain	0.8800
19:51822848:T:G	donor_gain	0.8800
19:51816989:T:TA	acceptor_gain	0.8500
19:51822794:A:T	donor_gain	0.8400
19:51795312:G:GT	donor_gain	0.8000

AlphaMissense

2336 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:51824021:G:C	W91C	0.993
19:51824021:G:T	W91C	0.993
19:51824019:T:A	W91R	0.991
19:51824019:T:C	W91R	0.991
19:51824376:T:C	F210L	0.977
19:51824378:C:A	F210L	0.977
19:51824378:C:G	F210L	0.977
19:51824040:T:A	C98S	0.975
19:51824041:G:C	C98S	0.975
19:51824496:T:C	F250L	0.973
19:51824498:C:A	F250L	0.973
19:51824498:C:G	F250L	0.973
19:51823984:C:G	P79R	0.970
19:51823880:T:A	N44K	0.969
19:51823880:T:G	N44K	0.969
19:51823971:A:C	S75R	0.969
19:51823973:T:A	S75R	0.969
19:51823973:T:G	S75R	0.969
19:51824276:T:G	C176W	0.969
19:51824274:T:A	C176S	0.968
19:51824275:G:C	C176S	0.968
19:51824631:A:C	S295R	0.968
19:51824633:C:A	S295R	0.968
19:51824633:C:G	S295R	0.968
19:51824196:T:A	W150R	0.967
19:51824196:T:C	W150R	0.967
19:51824082:A:C	S112R	0.966
19:51824084:T:A	S112R	0.966
19:51824084:T:G	S112R	0.966
19:51823961:C:A	D71E	0.962

dbSNP variants (sampled 300 via entrez): RS1000029854 (19:51814204 T>C), RS1000325392 (19:51820648 G>A,C), RS1000369472 (19:51796193 G>T), RS1000468745 (19:51801122 G>A,T), RS1000508464 (19:51815866 AAAAAAG>A), RS1000567317 (19:51798329 G>A), RS1000671429 (19:51803474 C>T), RS1000810332 (19:51807586 T>C), RS1000854691 (19:51797037 C>A), RS1000897721 (19:51802780 T>C), RS1000968561 (19:51797307 C>A), RS1001040854 (19:51815543 T>C), RS1001170675 (19:51799266 G>A), RS1001186391 (19:51813076 G>A), RS1001426566 (19:51794368 G>T)

Disease associations

OMIM: gene MIM:136539 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

20 associations (top):

Study	Trait	p-value
GCST004623_39	Neutrophil percentage of granulocytes	7.000000e-09
GCST004866_7	Alopecia areata	6.000000e-06
GCST005531_84	Multiple sclerosis	3.000000e-06
GCST005760_1	Dimensional psychopathology (Cognitive)	3.000000e-08
GCST006611_77	HDL cholesterol	3.000000e-11
GCST007277_24	Tourette syndrome	9.000000e-07
GCST008070_7	HDL cholesterol levels	2.000000e-06
GCST008075_116	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	8.000000e-16
GCST008075_56	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	2.000000e-12
GCST008084_229	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	1.000000e-18
GCST008084_7	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	9.000000e-16
GCST008085_109	HDL cholesterol levels in current drinkers	4.000000e-06
GCST008085_166	HDL cholesterol levels in current drinkers	1.000000e-08
GCST010043_75	Asthma	3.000000e-08
GCST010241_62	Apolipoprotein A1 levels	3.000000e-14
GCST010242_6	HDL cholesterol levels	8.000000e-18
GCST010796_4981	Electrocardiogram morphology (amplitude at temporal datapoints)	1.000000e-08
GCST90002381_356	Eosinophil count	3.000000e-18
GCST90002382_526	Eosinophil percentage of white cells	1.000000e-18
GCST90002399_445	Neutrophil percentage of white cells	8.000000e-10

EFO canonical traits (9, from GWAS)

EFO ID	Trait name
EFO:0007994	neutrophil percentage of granulocytes
EFO:0009098	cognitive domain measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004329	alcohol drinking
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004327	electrocardiography
EFO:0004842	eosinophil count
EFO:0007991	eosinophil percentage of leukocytes
EFO:0007990	neutrophil percentage of leukocytes

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5646 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

10 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 79,309 (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
CHEMBL1200492	NEFAZODONE HYDROCHLORIDE	4	5,428
CHEMBL1200776	CINACALCET HYDROCHLORIDE	4	1,220
CHEMBL1263	SALMETEROL	4	40,383
CHEMBL1615374	VILAZODONE HYDROCHLORIDE	4	432
CHEMBL398435	TICAGRELOR	4	2,956
CHEMBL567	PERPHENAZINE	4	21,883
CHEMBL506981	REMINERTANT	3	235
CHEMBL232656	BX 471 FREE BASE	2	191
CHEMBL267777	RITANSERIN	2	4,779
CHEMBL405355	NIGULDIPINE	2	1,802

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Formylpeptide receptors

Most potent curated ligand interactions (9 total), top 9:

Ligand	Action	Affinity	Parameter
humanin	Full agonist	8.95	pEC50
LXA4	Full agonist	8.82	pKd
WKYMVm	Full agonist	8.52	pEC50
F2L	Full agonist	8.2	pEC50
F2L-[125I]Tyr	Full agonist	8.0	pKd
annexin I-(2-26)	Full agonist	7.0	pEC50
fMet-Met-Tyr-Ala-Leu-Phe	Full agonist	6.0	pEC50
WRWWWW	Antagonist	6.0	pIC50
Hp(2-20)	Full agonist	5.0	pEC50

ChEMBL bioactivities

415 potent at pChembl≥5 of 428 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.42	EC50	3.8	nM	CHEMBL3728341
8.18	EC50	6.6	nM	CHEMBL3733191
8.13	EC50	7.4	nM	CHEMBL3730664
8.00	EC50	10	nM	CHEMBL552527
7.92	EC50	12	nM	CHEMBL3731635
7.89	EC50	13	nM	CHEMBL3730156
7.82	EC50	15	nM	CHEMBL3731671
7.82	EC50	15	nM	CHEMBL3731035
7.82	EC50	15	nM	CHEMBL3728830
7.80	EC50	16	nM	CHEMBL3728649
7.80	EC50	16	nM	CHEMBL3731316
7.75	EC50	18	nM	CHEMBL3730919
7.70	EC50	20	nM	CHEMBL3731064
7.58	EC50	26	nM	CHEMBL3733261
7.57	EC50	27	nM	CHEMBL3732345
7.57	EC50	27	nM	CHEMBL3731822
7.55	EC50	28	nM	CHEMBL3732539
7.54	EC50	29	nM	CHEMBL3729493
7.52	EC50	30	nM	CHEMBL3728150
7.50	EC50	32	nM	CHEMBL3729722
7.48	EC50	33	nM	CHEMBL3732902
7.39	EC50	41	nM	CHEMBL3729460
7.36	EC50	44	nM	CHEMBL3729342
7.34	EC50	46	nM	CHEMBL3728769
7.33	EC50	47	nM	CHEMBL3728352
7.28	EC50	52	nM	CHEMBL3732978
7.24	EC50	57	nM	CHEMBL3727697
7.24	EC50	58	nM	CHEMBL3730217
7.22	EC50	60	nM	CHEMBL3730955
7.21	EC50	61	nM	CHEMBL3729805
7.21	EC50	62	nM	CHEMBL3730330
7.19	EC50	65	nM	CHEMBL3728125
7.19	EC50	64	nM	CHEMBL3731680
7.18	EC50	66	nM	CHEMBL3729273
7.17	EC50	68	nM	CHEMBL3731599
7.17	EC50	67	nM	CHEMBL3728119
7.17	EC50	67	nM	CHEMBL3728646
7.15	EC50	71	nM	CHEMBL3732566
7.14	EC50	72	nM	CHEMBL3728781
7.13	EC50	74	nM	CHEMBL3730257
7.12	EC50	75	nM	CHEMBL3733287
7.10	EC50	79	nM	CHEMBL3732885
7.05	EC50	89	nM	CHEMBL3733253
7.04	EC50	91	nM	CHEMBL3732281
7.04	EC50	91	nM	CHEMBL3727450
7.03	EC50	94	nM	CHEMBL3729633
7.03	EC50	94	nM	CHEMBL3732163
7.02	EC50	95	nM	CHEMBL3730159
7.00	EC50	100	nM	CHEMBL3728511
7.00	EC50	99	nM	CHEMBL3730922

PubChem BioAssay actives

2 with measured affinity, of 99 total; 2 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
(2S)-6-amino-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]hexanamide	428659: Agonist activity at FPRL2 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay	ec50	0.0100	uM
(2S)-2-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	428659: Agonist activity at FPRL2 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay	ec50	1.9000	uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
aflatoxin B2	increases methylation	1
nickel sulfate	increases expression	1
S-(1,2-dichlorovinyl)cysteine	increases expression, affects response to substance	1
CGP 52608	affects binding, increases reaction	1
beta-hydroxy simvastatin acid	increases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Calcitriol	decreases expression	1
Doxorubicin	decreases expression	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression	1
Nickel	increases expression	1
Aflatoxin B1	decreases methylation	1
Antirheumatic Agents	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

8 unique, capped per target: 4 functional, 4 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1051691	Functional	Agonist activity at FPRL2 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay	6-methyl-2,4-disubstituted pyridazin-3(2H)-ones: a novel class of small-molecule agonists for formyl peptide receptors. — J Med Chem
CHEMBL2393753	Binding	Agonist activity at FPR3 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization relative to WKYMVm	Further studies on 2-arylacetamide pyridazin-3(2H)-ones: design, synthesis and evaluation of 4,6-disubstituted analogs as formyl peptide receptors (FPRs) agonists. — Eur J Med Chem

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_KV16	cAMP Hunter CHO-K1 FPR3 Gi	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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