FPR1

Summary

FPR1 (formyl peptide receptor 1, HGNC:3826) is a protein-coding gene on chromosome 19q13.41, encoding N-formyl peptide receptor 1 (P21462). Pattern recognition G-protein coupled receptor (PRR/GPCR) involved in innate recognition of N-formyl-methionyl peptides derived from invading microbes and host mitochondria as pathogen- and damage-associated molecular patterns (PAMPs and DAMPs).

This gene encodes a G protein-coupled receptor of mammalian phagocytic cells that is a member of the G-protein coupled receptor 1 family. The protein mediates the response of phagocytic cells to invasion of the host by microorganisms and is important in host defense and inflammation.

Source: NCBI Gene 2357 — RefSeq curated summary.

At a glance

• Gene–disease (curated): susceptibility to localized juvenile periodontitis (Supportive, GenCC) — +1 more curated relationship
• GWAS associations: 8
• Clinical variants (ClinVar): 269 total
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002029

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3826
Approved symbol	FPR1
Name	formyl peptide receptor 1
Location	19q13.41
Locus type	gene with protein product
Status	Approved
Aliases	FPR, FMLP
Ensembl gene	ENSG00000171051
Ensembl biotype	protein_coding
OMIM	136537
Entrez	2357

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 11 protein_coding

ENST00000304748, ENST00000594900, ENST00000595042, ENST00000600815, ENST00000881808, ENST00000881809, ENST00000881810, ENST00000930484, ENST00000948394, ENST00000948395, ENST00000948396

RefSeq mRNA: 2 — MANE Select: NM_002029 NM_001193306, NM_002029

CCDS: CCDS12839

Canonical transcript exons

ENST00000304748 — 2 exons

Exon	Start	End
ENSE00003151376	51745773	51747005
ENSE00003218269	51751814	51751878

Expression profiles

Bgee: expression breadth ubiquitous, 215 present calls, max score 99.52.

FANTOM5 (CAGE): breadth broad, TPM avg 44.4500 / max 8219.9604, expressed in 561 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
182480	44.1000	558
182478	0.0921	41
182491	0.0757	40
182492	0.0634	34
182479	0.0604	13
182490	0.0584	36

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
blood	UBERON:0000178	99.52	gold quality
monocyte	CL:0000576	99.20	gold quality
leukocyte	CL:0000738	99.13	gold quality
mononuclear cell	CL:0000842	99.12	gold quality
periodontal ligament	UBERON:0008266	99.01	gold quality
granulocyte	CL:0000094	98.95	gold quality
trabecular bone tissue	UBERON:0002483	97.57	gold quality
spleen	UBERON:0002106	96.93	gold quality
bone marrow	UBERON:0002371	96.66	gold quality
right lung	UBERON:0002167	96.37	gold quality
upper lobe of left lung	UBERON:0008952	94.42	gold quality
bone marrow cell	CL:0002092	94.00	gold quality
upper lobe of lung	UBERON:0008948	93.96	gold quality
lower lobe of lung	UBERON:0008949	92.32	gold quality
vermiform appendix	UBERON:0001154	89.27	gold quality
gall bladder	UBERON:0002110	88.20	gold quality
lung	UBERON:0002048	86.96	gold quality
left uterine tube	UBERON:0001303	86.67	gold quality
descending thoracic aorta	UBERON:0002345	86.09	gold quality
omental fat pad	UBERON:0010414	84.95	gold quality
peritoneum	UBERON:0002358	84.91	gold quality
adipose tissue of abdominal region	UBERON:0007808	84.54	gold quality
thoracic aorta	UBERON:0001515	83.54	gold quality
ascending aorta	UBERON:0001496	83.18	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	83.13	gold quality
right coronary artery	UBERON:0001625	83.06	gold quality
left coronary artery	UBERON:0001626	83.05	gold quality
cranial nerve II	UBERON:0000941	81.85	gold quality
decidua	UBERON:0002450	81.76	silver quality
coronary artery	UBERON:0001621	81.52	gold quality

Single-cell (SCXA)

Detected in 14 experiment(s), a significant marker in 14.

Experiment	Marker?	Max mean expression
E-MTAB-9801	yes	1991.18
E-CURD-122	yes	75.25
E-HCAD-1	yes	67.76
E-GEOD-135922	yes	48.98
E-GEOD-84465	yes	40.76
E-MTAB-9221	yes	30.44
E-ANND-3	yes	28.50
E-MTAB-6701	yes	26.62
E-CURD-112	yes	26.36
E-MTAB-6678	yes	25.34
E-HCAD-10	yes	16.98
E-MTAB-9067	yes	13.66
E-CURD-88	yes	12.61
E-MTAB-8498	yes	10.03

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): IRF6, SPI1

miRNA regulators (miRDB)

11 targeting FPR1, 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-4481	100.00	66.42	1669
HSA-MIR-4745-5P	99.98	65.95	1028
HSA-MIR-4713-5P	99.78	67.80	1794
HSA-MIR-4502	99.65	66.99	1021
HSA-MIR-4761-5P	99.51	66.69	804
HSA-MIR-6165	99.44	67.12	1389
HSA-MIR-500A-5P	98.76	69.13	1241
HSA-MIR-6867-3P	98.12	66.07	1305
HSA-MIR-3192-5P	96.98	65.76	1926
HSA-MIR-4300	95.85	64.56	1003
HSA-MIR-5591-5P	95.85	64.76	1002

Literature-anchored findings (GeneRIF, showing 40)

• A conformational study of human fMLP (PMID:11860029)
• 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)
• phosphorylation domains differentially regulate arrestin and agonist affinity (PMID:12424254)
• Critical role of N-terminal N-glycosylation for proper folding of the formyl peptide receptor. (PMID:12565836)
• Six single nucleotide polymorphisms have been identified including two located in the FPR1 second extracellular loop that are significantly associated with the periodontitis phenotype in African-American patients. (PMID:12595898)
• Expression of FPRs on transformed or normal fibroblasts indicates that they are able to induce intracellular signaling events leading to fibroblast motility. (PMID:12902510)
• 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)
• FPR-F110S displayed a delayed and significantly reduced ERK phosphorylation whereas FPR-FSCW nearly lost the ability to phosphorylate ERK (PMID:15195697)
• FPR and FPRL1, use distinct signaling pathways in activation of human neutrophils (PMID:15625007)
• endogenous formyl peptides, released by eukaryotic mitochondria from necrotic cells, induce chemotaxis using formyl peptide receptors expressed by thrombin-activated platelets (PMID:15661400)
• urokinase receptor-derived SRSRY peptide regulates cross-talk between fMLP and vitronectin receptors (PMID:15866865)
• FPR is expressed by highly malignant human glioma cells and appears to mediate motility, growth, and angiogenesis of human glioblastoma by interacting with host-derived agonists. (PMID:15928303)
• Activation of the formyl peptide receptor inhibits lipopolysaccharide-induced dendritic cell maturation. (PMID:16002663)
• FPR-mediated activation of ERK1/2 takes place primarily through G protein and is physiologically important to ensure transcriptional activation of myeloid immunomodulators, such as cytokines. (PMID:16038804)
• Three distinct segments of the formyl peptide receptor 1 (FPR1) mRNA of Man share probabilistically significant homologies with segments of the 18S rRNA which are highly conserved from Drosophila to Man. (PMID:16114510)
• ERK/PLD2 pathway contributes to fMLP-mediated oxidant production (PMID:16253958)
• A model with additional receptor state is sufficient to describe response data when two ligands (agonist/agonist or agonist/antagonist pairs) are added simultaneously, suggesting that cells respond to the accumulation of active receptors. (PMID:16530386)
• AnxA1 has a role in stimulating SKCO-15 cell migration through nFPR activation (PMID:16675446)
• data suggest an increased receptor activity and phenotypic expression of increased inflammatory indices in subjects with the FPR1 p.T11 allele (PMID:16953235)
• The N-formyl peptide receptors present in MSCs may play an important role in signaling stem cell adhesion, migration, and homing to injured and inflamed tissue for repair. (PMID:17234990)
• the plasma membrane distributions of FPR and its cross-talk with IGE receptor (PMID:17267694)
• A new (patho)physiological role of FPR and its ligands in regulating MSC trafficking during induction of injured tissue repair. (PMID:17442310)
• Piroxicam inhibits the neutrophil responses triggered through formyl peptide receptor, but not through formyl peptide receptor like 1 and this inhibition is due to a reduced binding of the activating ligand to its cell surface receptor. (PMID:17692291)
• Polymorphonuclear neutrophils from subjects carrying the -12915T allele expressed significantly lower levels of FPR1 transcripts than those homozygous for the -12915C allele. (PMID:17927965)
• Theses results support a novel role for FPR stimulation in enhancing intestinal epithelial cell restitution through PI3K-dependent activation of Rac1 and Cdc42. (PMID:18056353)
• The predominant activation of ERK1/2 through G protein may be a common characteristic among chemoattractant receptors. (PMID:18060741)
• Formyl peptide receptor haplotypes do not appear to be associated with rheumatoid arthritis (PMID:18253729)
• The amino acid content in the N-terminal half of the cytoplasmic tail influences the structure and desensitization of FPR. (PMID:18952127)
• increased methylation of p53 gene retains human glioblastoma cells at a more poorly differentiated phase associated with the aberrant expression of FPR as a tumor-promoting cell surface receptor. (PMID:19037090)
• SAA stimulates CCL2 production via FPRL1 and, thus, contributes to atherosclerosis. (PMID:19167353)
• The frequency of synonymous SNP c.348T>C was significantly higher in African Americans with AgP than in controls. The 348T allele was significantly associated with AgP. (PMID:19254133)
• Signals evoked via the FPR caused unidirectional down-regulation of CCR3-mediated chemotaxis but not respiratory burst in human eosinophils. (PMID:19414538)
• The FPR1 single nucleotide polymorphism may be associated with E-selectin levels in the French population. (PMID:19530962)
• 348T/T genotype is associated with significantly impaired PMN chemotaxis and an increased risk for developing AgP in African Americans. These associations do not seem to be related to significant reductions in FPR1 transcripts in subjects expressing 348T. (PMID:19722801)
• Human natural killer (NK) cells express FPR1, and in turn the activation of the FPR1 receptor elicits cytolytic activity and chemotactic migration by interleukin-2 stimulated NK cells. (PMID:19843937)
• The presence of the C(+) genotype/allele C of FPR301 together with smoking conferred a higher risk for aggressive periodontitis. (PMID:20019777)
• The expression of FPR is responsible for increased motility of human glioblastoma cells and their formation of highly invasive tumours. (PMID:20197768)
• These observations suggest a novel signaling role for ANXA1 in mitogen-activated proliferation of breast tumor epithelial cells that is mediated via activation of FPR1 and FPR2. (PMID:20930115)
• When normotensive individuals were compared to hypertensives ones, similar FPR1 C32T genotypes and allele frequency distributions were found (PMID:21144844)
• This is the first study to evaluate polymorphisms of the FPR1 gene in stomach cancer to find a positive association between these polymorphisms and stomach cancer. (PMID:21216225)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Fpr1	ENSMUSG00000045551
rattus_norvegicus	Fpr1	ENSRNOG00000011174

Paralogs (8): C5AR2 (ENSG00000134830), GPR32 (ENSG00000142511), FPR2 (ENSG00000171049), C3AR1 (ENSG00000171860), CMKLR1 (ENSG00000174600), FPR3 (ENSG00000187474), C5AR1 (ENSG00000197405), GPR33 (ENSG00000214943)

Protein

Protein identifiers

N-formyl peptide receptor 1 — P21462 (reviewed: P21462)

Alternative names: N-formylpeptide chemoattractant receptor, fMet-Leu-Phe receptor

All UniProt accessions (3): P21462, M0QZT0, M0R315

UniProt curated annotations — full annotation on UniProt →

Function. Pattern recognition G-protein coupled receptor (PRR/GPCR) involved in innate recognition of N-formyl-methionyl peptides derived from invading microbes and host mitochondria as pathogen- and damage-associated molecular patterns (PAMPs and DAMPs). Functions as a sensor of PAMPs and DAMPs released upon microbial infection or tissue damage, triggering immune cell activation and chemotaxis to eliminate pathogens and restore tissue homeostasis. 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. Displays two affinity states for peptide agonists, low and high, likely accounting for selective signaling of myeloid cell functions at different phases of the inflammatory response. Subnanomolar concentrations of peptide agonists induce myeloid cell chemotaxis, whereas micromolar concentrations trigger degranulation and superoxide production. May recognize a myriad of bacterial signal peptides indicative of an evolutionary conserved detection mechanism in host defense against bacterial infection. Triggers bactericidal functions of neutrophils and phagocytes in response to N-formyl-Met-Leu-Phe (fMLF) which is part of the signal peptide sequences of hundreds distinct bacterial strains. In the homeostatic wound healing response to tissue injury, senses ’necrotaxis’ DAMP-type signals released in the form of mitochondria-derived N-formylated peptides and guides neutrophil trafficking toward necrotic cells within the injury site. In the context of antitumor immunity, interacts with ANXA1 and guides dendritic cell positioning in close proximity to necrotic tumor cells, allowing for tumor-associated antigen uptake and cross-presentation to T cells. Receptor for TAFA4, mediates its effects on chemoattracting macrophages, promoting phagocytosis and increasing reactive oxygen species (ROS) release. Receptor for cathepsin CTSG, leading to increased phagocyte chemotaxis. Beyond canonical N-terminal formylated peptide agonists, can also be activated by C-terminal amidated peptides, which appear to all share a tripartite structure motif oriented around a carboxyl group. Differential signaling is also defined by receptor oligomerization state. Pro-resolving ligands, such as lipoxin A4 or ANXA1, induce the formation of FPR1:FPR2 heterodimers triggering proapoptotic JNK pathway in neutrophils. (Microbial infection) Used by Y. pestis as a receptor on human immune cells. Upon infection, Y. pestis releases N-formyl peptides that activate FPR1-mediated immune signaling and chemotaxis. This leads to Y. pestis docking on FPR1 via the lcrV needle cap protein of its type III secretion system (T3SS) followed by the delivery of effector proteins into host immune cells, ultimately triggering immune cell apoptosis.

Subunit / interactions. (Microbial infection) Interacts with S.aureus chemotaxis inhibitory protein (CHIPS); the interaction blocks the receptor and may thus inhibit the immune response. (Microbial infection) Interacts with lcrV, the needle cap protein of the Y. pestis type III secretion system; this interaction promotes the translocation of bacterial effectors into host immune cells including neutrophils, macrophages and dendritic cells, thus targeting them for destruction. Homodimer. Heterodimer with FPR2 or FPR3; the heterodimerization with FPR2 is potentiated in response to anti-inflammatory agonists such as lipoxin A4 and ANXA1. Forms a complex with heterotrimeric G(i) protein composed of GNAI1, GNB1 and GNG2 subunits.

Subcellular location. Cell membrane.

Tissue specificity. Monocytes (at protein level). Neutrophils.

Post-translational modifications. Phosphorylated; which is necessary for desensitization.

Polymorphism. Common FPR1 variations may have been selected to enhance human resistance to infections. FRP1 p.Arg190Trp is identified as an allele that protect neutrophils from destruction by Y. pestis type III secretion system.

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

RefSeq proteins (2): NP_001180235, NP_002020* (*=MANE)

Domains & families (InterPro)

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

Pfam: PF00001

Enzyme classification (BRENDA):

• EC 3.1.4.4 — phospholipase D (BRENDA: 94 organisms, 465 substrates, 320 inhibitors, 67 Km, 27 kcat entries)

Substrate kinetics (BRENDA)

21 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
PHOSPHATIDYLCHOLINE	0.0015–2.5	18
N-PALMITOYL-PHOSPHATIDYLETHANOLAMINE	0.0029–0.045	16
DIOLEOYL-PHOSPHATIDYLCHOLINE	0.0015–3	4
LYSOPHOSPHATIDYLCHOLINE	1–3	4
EGG PHOSPHATIDYLCHOLINE	30.2–33.17	2
L-ALPHA-PHOSPHATIDYLCHOLINE	2.71–3.44	2
PHOSPHATIDYL-P-NITROPHENOL	0.075–1.16	2
PHOSPHATIDYLETHANOLAMINE	0.91–4	2
1,2-DIBUTYL-SN-GLYCERO-3-PHOSPHOCHOLINE	0.16	1
1-PALMITOYL-2-OLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE	0.271	1
BIS(P-NITROPHENYL)PHOSPHATE	0.6	1
DIBUTYROYLPHOSPHATIDYLCHOLINE	0.2	1
DIHEPTANOYLPHOSPHATIDYLCHOLINE	0.23	1
DIHEXANOYLPHOSPHATIDYLCHOLINE	2.64	1
DIPALMITOYLPHOSPHATIDYLCHOLINE	0.78	1

UniProt features (79 total): mutagenesis site 16, helix 13, binding site 11, topological domain 8, modified residue 8, transmembrane region 7, sequence variant 5, glycosylation site 2, turn 2, strand 2, chain 1, region of interest 1, compositionally biased region 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
7VFX	ELECTRON MICROSCOPY	2.8
7EUO	ELECTRON MICROSCOPY	2.9
9KFT	ELECTRON MICROSCOPY	3.06
7T6T	ELECTRON MICROSCOPY	3.2
7WVU	ELECTRON MICROSCOPY	3.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P21462-F1	84.17	0.57

Antibody-complex structures (SAbDab): 3 — 7EUO, 7VFX, 9KFT

Functional residue map

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

Ligand- & substrate-binding residues (11): 106; 106; 201; 201; 201; 205; 205; 205; 257; 257; 257

Post-translational modifications (8): 328, 329, 331, 332, 334, 336, 338, 339

Disulfide bonds (1): 98–176

Glycosylation sites (2): 4, 10

Mutagenesis-validated functional residues (16):

Position	Phenotype
81	slightly decreases intracellular camp reduction upon stimulation with n-formylated fmlf peptide.
84	decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlfii.
102	slightly decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlf. slightly decreases the agon
102	decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlfii.
106	abolishes the response to n-formyl peptides fmlf, fmifl and fmlfii.
106	abolishes the response to n-formyl peptides fmlf and fmifl.
109	slightly decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlf. decreases the agonist poten
110	slightly decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlf.
178	decreases the agonist potency of non-formylated wkymvm peptide.
201	abolishes the response to n-formyl peptide fmlf. decreases intracellular camp reduction upon stimulation with n-formyl p
205	abolishes the response to n-formyl peptide fmlf. decreases intracellular camp reduction upon stimulation with n-formyl p
257	decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlfii.
265	decreases the agonist potency of non-formylated wkymvm peptide.
277	no significant effect on intracellular camp reduction upon stimulation with n-formyl peptide fmlfii.
283	no significant effect on intracellular camp reduction upon stimulation with n-formyl peptide fmlf.
291	slightly decreases intracellular camp reduction upon stimulation with n-formyl peptide fmlf.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-418594	G alpha (i) signalling events
R-HSA-444473	Formyl peptide receptors bind formyl peptides and many other ligands
R-HSA-6783783	Interleukin-10 signaling
R-HSA-6798695	Neutrophil degranulation

MSigDB gene sets: 265 (showing top): BIOCARTA_FMLP_PATHWAY, REACTOME_INNATE_IMMUNE_SYSTEM, MCLACHLAN_DENTAL_CARIES_UP, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOCC_VACUOLAR_MEMBRANE, GOCC_SECRETORY_GRANULE, MODULE_64, MODULE_128, IVANOVA_HEMATOPOIESIS_MATURE_CELL, AMIT_SERUM_RESPONSE_40_MCF10A, MODULE_173, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_TAXIS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS

GO Biological Process (11): complement receptor mediated signaling pathway (GO:0002430), chemotaxis (GO:0006935), inflammatory response (GO:0006954), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), obsolete nitric oxide mediated signal transduction (GO:0007263), cell communication (GO:0007154), signaling (GO:0023052)

GO Molecular Function (7): G protein-coupled receptor binding (GO:0001664), complement receptor activity (GO:0004875), G protein-coupled receptor activity (GO:0004930), N-formyl peptide receptor activity (GO:0004982), scavenger receptor binding (GO:0005124), RAGE receptor binding (GO:0050786), protein binding (GO:0005515)

GO Cellular Component (6): cytoplasm (GO:0005737), plasma membrane (GO:0005886), membrane (GO:0016020), secretory granule membrane (GO:0030667), azurophil granule membrane (GO:0035577), ficolin-1-rich granule membrane (GO:0101003)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
GPCR downstream signalling	1
Peptide ligand-binding receptors	1
Signaling by Interleukins	1
Innate Immune System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
signaling receptor binding	3
cellular process	2
transmembrane signaling receptor activity	2
cellular anatomical structure	2
secretory granule membrane	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
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase activity	1
phospholipase C activator activity	1
regulation of biological quality	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
intracellular anatomical structure	1
membrane	1
cell periphery	1
secretory granule	1
cytoplasmic vesicle membrane	1
bounding membrane of organelle	1
lysosomal membrane	1
azurophil granule	1
tertiary granule	1
ficolin-1-rich granule	1

Protein interactions and networks

STRING

1626 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FPR1	ANXA1	P04083	998
FPR1	TREM1	Q9NP99	784
FPR1	SAG	P10523	762
FPR1	TLR9	Q9NR96	718
FPR1	TLR8	Q9NR97	673
FPR1	GNAI2	P04899	657
FPR1	TLR4	O00206	643
FPR1	CXCL8	P10145	641
FPR1	IL1B	P01584	632
FPR1	TNF	P01375	616
FPR1	SAA1	P02735	606
FPR1	TREM2	Q9NZC2	598
FPR1	CCL2	P13500	589
FPR1	SAA1	P02735	585
FPR1	CXCR1	P25024	566

IntAct

14 interactions, top by confidence:

A	B	Type	Score
MAPK13	FPR1	psi-mi:“MI:0915”(physical association)	0.500
GRK2	FPR1	psi-mi:“MI:0915”(physical association)	0.500
FPR1	MAPK13	psi-mi:“MI:0914”(association)	0.500
MAPK3	FPR1	psi-mi:“MI:0915”(physical association)	0.400
FPR1	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
FPR1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
FPR1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
FPR1	GPR89A	psi-mi:“MI:0914”(association)	0.350
FPR1	RAB29	psi-mi:“MI:0914”(association)	0.350
FPR1	NBAS	psi-mi:“MI:0914”(association)	0.350
lcrD	FPR1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (142): PIK3CG (Phenotypic Enhancement), PIK3R5 (Phenotypic Enhancement), FPR1 (Affinity Capture-Western), AGER (Affinity Capture-Western), XPO6 (Affinity Capture-MS), TTI1 (Affinity Capture-MS), IPO13 (Affinity Capture-MS), FASTKD1 (Affinity Capture-MS), CNOT8 (Affinity Capture-MS), COG6 (Affinity Capture-MS), ATL2 (Affinity Capture-MS), COG1 (Affinity Capture-MS), ERAP1 (Affinity Capture-MS), ANKRD44 (Affinity Capture-MS), SYNGR2 (Affinity Capture-MS)

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

12 interactions.

A	Effect	B	Mechanism
FPR1	“up-regulates activity”	GNAI1	binding
FPR1	“up-regulates activity”	GNAI3	binding
FPR1	“up-regulates activity”	GNA14	binding
N-formyl-L-methionyl-L-leucyl-L-phenylalanine	“up-regulates activity”	FPR1	“chemical activation”
ANXA1	“up-regulates activity”	FPR1	binding
GRK2	“down-regulates activity”	FPR1	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	157
Likely benign	89
Benign	18

Top pathogenic / likely-pathogenic (0)

SpliceAI

664 predictions. Top by Δscore:

Variant	Effect	Δscore
19:51747003:CTC:C	acceptor_gain	1.0000
19:51747006:C:CC	acceptor_gain	1.0000
19:51751811:TACC:T	donor_loss	1.0000
19:51751812:ACCTG:A	donor_loss	1.0000
19:51751813:C:G	donor_loss	1.0000
19:51747001:TGCTC:T	acceptor_gain	0.9900
19:51747004:TC:T	acceptor_gain	0.9900
19:51747004:TCCTG:T	acceptor_loss	0.9900
19:51747005:CC:C	acceptor_gain	0.9900
19:51747005:CCTG:C	acceptor_loss	0.9900
19:51747006:CT:C	acceptor_loss	0.9900
19:51747007:T:G	acceptor_loss	0.9900
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
19:51751812:A:AC	donor_gain	0.9800
19:51751813:C:CC	donor_gain	0.9800
19:51761227:GCTG:G	donor_gain	0.9800
19:51763442:A:G	donor_gain	0.9800
19:51768638:GTTTC:G	acceptor_loss	0.9800
19:51768639:TTTCA:T	acceptor_loss	0.9800
19:51768640:TTCAG:T	acceptor_loss	0.9800
19:51768641:TCAGG:T	acceptor_loss	0.9800
19:51768642:CAGGT:C	acceptor_loss	0.9800
19:51768643:A:AG	acceptor_gain	0.9800
19:51768643:A:T	acceptor_loss	0.9800
19:51768644:G:GG	acceptor_gain	0.9800

AlphaMissense

2286 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:51746722:C:A	W91C	0.994
19:51746722:C:G	W91C	0.994
19:51746245:A:C	F250L	0.992
19:51746245:A:T	F250L	0.992
19:51746247:A:G	F250L	0.992
19:51746365:G:C	F210L	0.992
19:51746365:G:T	F210L	0.992
19:51746367:A:G	F210L	0.992
19:51746724:A:G	W91R	0.989
19:51746724:A:T	W91R	0.989
19:51746468:C:G	C176S	0.988
19:51746469:A:T	C176S	0.988
19:51746113:G:C	S294R	0.987
19:51746113:G:T	S294R	0.987
19:51746115:T:G	S294R	0.987
19:51746467:G:C	C176W	0.987
19:51746469:A:G	C176R	0.986
19:51746702:C:G	C98S	0.986
19:51746703:A:T	C98S	0.986
19:51746468:C:T	C176Y	0.984
19:51746362:G:C	S211R	0.983
19:51746362:G:T	S211R	0.983
19:51746364:T:G	S211R	0.983
19:51746782:G:C	D71E	0.983
19:51746782:G:T	D71E	0.983
19:51746702:C:T	C98Y	0.982
19:51746863:G:C	N44K	0.982
19:51746863:G:T	N44K	0.982
19:51746877:C:G	G40R	0.982
19:51746877:C:T	G40R	0.982

dbSNP variants (sampled 300 via entrez): RS1000001897 (19:51747925 G>A), RS1000115081 (19:51747594 G>A), RS1000400153 (19:51752390 A>T), RS1001006253 (19:51749341 A>C), RS1001120239 (19:51749133 T>A,C), RS1001345032 (19:51753845 C>G), RS1001909024 (19:51749688 GTCTC>G,GTCTCTC), RS1002249473 (19:51749384 A>T), RS1002827776 (19:51749437 C>T), RS1002928292 (19:51745544 A>G), RS1003044286 (19:51745816 G>T), RS1003319780 (19:51750929 G>A), RS1003423420 (19:51750622 G>T), RS1003865680 (19:51745414 C>T), RS1004483101 (19:51750436 C>G)

Disease associations

OMIM: gene MIM:136537 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
susceptibility to localized juvenile periodontitis	Supportive	Autosomal recessive
Tourette syndrome	No Known Disease Relationship	Unknown

Mondo (5): gingival disorder (MONDO:0002021), prostate cancer (MONDO:0008315), periodontitis (MONDO:0005076), Tourette syndrome (MONDO:0007661), susceptibility to localized juvenile periodontitis (MONDO:0018643)

Orphanet (1): Familial prostate cancer (Orphanet:1331)

HPO phenotypes

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

GWAS associations

8 associations (top):

Study	Trait	p-value
GCST004623_39	Neutrophil percentage of granulocytes	7.000000e-09
GCST004866_7	Alopecia areata	6.000000e-06
GCST007277_24	Tourette syndrome	9.000000e-07
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
GCST90002388_381	Lymphocyte count	5.000000e-10
GCST90002399_445	Neutrophil percentage of white cells	8.000000e-10

EFO canonical traits (6, from GWAS)

EFO ID	Trait name
EFO:0007994	neutrophil percentage of granulocytes
EFO:0004327	electrocardiography
EFO:0004842	eosinophil count
EFO:0007991	eosinophil percentage of leukocytes
EFO:0004587	lymphocyte count
EFO:0007990	neutrophil percentage of leukocytes

MeSH disease descriptors (4)

Descriptor	Name	Tree numbers
D005882	Gingival Diseases	C07.465.714.258
D010518	Periodontitis	C07.465.714.533
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750
D005879	Tourette Syndrome	C10.228.140.079.898; C10.228.662.825.800; C10.574.500.850; C16.320.400.820; F03.625.992.850

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3038479 (PROTEIN FAMILY), CHEMBL3359 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 192,589 (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
CHEMBL101	PHENYLBUTAZONE	4	59,455
CHEMBL1200681	MONTELUKAST SODIUM	4	10,913
CHEMBL1200776	CINACALCET HYDROCHLORIDE	4	1,220
CHEMBL1223	PENICILLIN G POTASSIUM	4	19,982
CHEMBL1471	APREPITANT	4	901
CHEMBL1707	LOPERAMIDE HYDROCHLORIDE	4	59,532
CHEMBL567	PERPHENAZINE	4	21,883
CHEMBL832	SULFINPYRAZONE	4	13,780
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL405355	NIGULDIPINE	2	1,802
CHEMBL4784510	BMS-986235	1	25

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 (39 total), top 25:

Ligand	Action	Affinity	Parameter
fMet-Ile-Phe-Leu	Full agonist	10.5	pEC50
fMet-Leu-Phe	Full agonist	10.2	pEC50
[3H]fMet-Leu-Phe	Full agonist	9.3	pKd
WKYMVm	Full agonist	9.0	pEC50
Met-Met-Trp-Leu-Leu	Full agonist	9.0	pEC50
fMet-Met-Trp-Leu-Leu	Full agonist	9.0	pEC50
fMet-Ile-Val-Ile-Leu	Full agonist	8.7	pEC50
compound 43 [PMID: 21173551]	Full agonist	8.7	pEC50
fMet-Ile-Val-Thr-Leu-Phe	Full agonist	8.6	pEC50
fMet-Leu-Phe-Ile-Ile-Lys-FITC	Full agonist	8.6	pKd
T20(DP178)	Full agonist	8.3	pEC50
fMet-Leu-Phe-Glu	Full agonist	8.2	pEC50
fMet-Met-Tyr-Ala-Leu-Phe	Full agonist	8.0	pEC50
AZ2158	Antagonist	7.7	pKd
[125I]CHIPS	Antagonist	7.5	pKd
AG-14	Full agonist	7.4	pEC50
cyclosporin H	Antagonist	7.1	pKi
[125I]cathepsin G (human)	Full agonist	7.0	pKd
BVT173187	Antagonist	7.0	pIC50
3570-0208 [PMID:19807662]	Antagonist	7.0	pKi
i-Boc-Met-Leu-Phe	Antagonist	6.6	pIC50
annexin I	Full agonist	6.6	pEC50
t-Boc-FLFLF	Antagonist	6.5	pKi
diamide 7	Antagonist	6.5	pIC50
BMS-986235	Agonist	6.4	pEC50

Binding affinities (BindingDB)

79 measured of 414 human assays (427 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
MLS000079917	EC50	0.0133 nM
2-(3-chlorophenyl)-4-N-methyltriazole-4,5-diamine	EC50	0.325 nM
WKFMVm-NH2	KI	18 nM
WKWMVm-NH2	KI	19 nM
(S)-2-[(R)-2-((S)-2-{(R)-2-[(S)-2-(3-Adamantan-1-yl-ureido)-3-phenyl-propionylamino]-4-methyl-pentanoylamino}-3-phenyl-propionylamino)-4-methyl-pentanoylamino]-3-phenyl-propionic acid	IC50	20 nM
WHYMVm-NH2	KI	32 nM
WKYMVm-NH2	KI	47 nM
WRYMVm-NH2	KI	55 nM
WKYM(F/W)m-NH2	KI	57 nM
WDYMVm-NH2	KI	99 nM
WKHMVm-NH2	KI	282 nM
WEYMVm-NH2	KI	323 nM
1-(4-chlorophenyl)-3-[(3S,4S)-4-(4-methoxyphenyl)-1-methyl-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3R,4R)-1-acetyl-4-(4-methoxyphenyl)piperidin-3-yl]-3-(6-chloro-3-pyridinyl)urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3R,4R)-1-acetyl-4-(4-methoxyphenyl)piperidin-3-yl]-3-pyrimidin-5-ylurea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
rac-trans-1-(1-acetyl-4-(4-methoxyphenyl)piperidin-3-yl)-3-(6-methylpyridin-3-yl)urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3R,4R)-1-acetyl-4-(4-methoxyphenyl)piperidin-3-yl]-3-[6-(trifluoromethyl)-3-pyridinyl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)piperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-1-(cyclopropanecarbonyl)-4-(2,6-difluoro-4-methoxyphenyl)piperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-4-(2-fluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-4-(2-fluoro-4-methoxyphenyl)piperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3R,4R)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]-3-pyridin-4-ylurea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]-3-pyridin-4-ylurea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(5-chlorothiophen-2-yl)-3-[(3R,4R)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(1-benzothiophen-2-yl)-3-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]-3-(3-methyl-1,2-thiazol-5-yl)urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(5-chloro-1,3-thiazol-2-yl)-3-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chloro-3-fluorophenyl)-3-[(3S,4S)-4-(2,6-difluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[4-(2-fluoro-4-methoxyphenyl)-1-(2-methoxyethyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[1-(2,2-difluoroethyl)-4-(2-fluoro-4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[4-(2,4-difluorophenyl)-1-(2-methoxyethyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[1-(2,2-difluoroethyl)-4-(2,4-difluorophenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[4-(2,4-difluorophenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-ethyl-2,6-difluorophenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-[4-(difluoromethoxy)-2,6-difluorophenyl]-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-methylsulfanylphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-ethylphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-[4-(difluoromethoxy)phenyl]-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-methylsulfonylphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-4-(4-methoxyphenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-4-phenylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-4-phenylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3R,4R)-1-(cyclopropanecarbonyl)-4-phenylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[(3S,4S)-1-(cyclopropanecarbonyl)-4-phenylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[2-(2,6-difluoro-4-methoxyphenyl)-1-methylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[2-(4-methoxyphenyl)-1-methylpiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
1-(4-chlorophenyl)-3-[4-(4-chlorophenyl)-6-oxopiperidin-3-yl]urea	EC50	500 nM	US-10265310: 6-membered cyclic amines or lactames substituted with urea and phenyl
YMVm-NH2	KI	567 nM
WKYMYm-NH2	KI	671 nM

ChEMBL bioactivities

1030 potent at pChembl≥5 of 1172 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.30	EC50	0.5	nM	CHEMBL5567096
9.25	EC50	0.56	nM	CHEMBL5543029
9.24	EC50	0.58	nM	CHEMBL5276622
9.23	EC50	0.59	nM	CHEMBL5558209
9.00	EC50	1	nM	CHEMBL267388
9.00	EC50	1	nM	CHEMBL7753
9.00	EC50	1	nM	CHEMBL5285824
9.00	EC50	1	nM	CHEMBL5267736
9.00	EC50	1	nM	CHEMBL5286200
9.00	EC50	1	nM	CHEMBL5290016
9.00	EC50	1	nM	CHEMBL5275766
9.00	EC50	1	nM	CHEMBL5276203
9.00	EC50	1	nM	CHEMBL5278464
9.00	EC50	0.99	nM	CHEMBL5958452
8.96	EC50	1.1	nM	CHEMBL5562287
8.92	EC50	1.2	nM	CHEMBL5862924
8.77	EC50	1.7	nM	CHEMBL5284816
8.70	IC50	2	nM	CHEMBL266802
8.70	EC50	2	nM	CHEMBL266802
8.70	IC50	2	nM	CHEMBL267388
8.70	IC50	2	nM	CHEMBL7753
8.70	EC50	2	nM	CHEMBL5560412
8.70	EC50	2	nM	CHEMBL6028833
8.68	Kd	2.1	nM	CHEMBL3311300
8.60	EC50	2.5	nM	CHEMBL285518
8.52	Kd	3	nM	N-FORMYLMETHIONYL-LEUCYLPHENYLALANINE
8.52	EC50	3	nM	CHEMBL5563648
8.52	EC50	3	nM	CHEMBL5560783
8.46	EC50	3.5	nM	N-FORMYLMETHIONYL-LEUCYLPHENYLALANINE
8.46	EC50	3.5	nM	CHEMBL6063100
8.43	EC50	3.687	nM	N-FORMYLMETHIONYL-LEUCYLPHENYLALANINE
8.41	EC50	3.9	nM	CHEMBL4744094
8.40	IC50	3.981	nM	CHEMBL1934424
8.33	EC50	4.7	nM	CHEMBL2336647
8.31	EC50	4.93	nM	CHEMBL5276878
8.31	EC50	4.9	nM	CHEMBL6016024
8.30	EC50	5	nM	CHEMBL5542212
8.30	EC50	5	nM	CHEMBL5813829
8.29	EC50	5.1	nM	CHEMBL6026791
8.24	EC50	5.8	nM	CHEMBL5837333
8.19	EC50	6.457	nM	CHEMBL4532583
8.16	Kd	6.9	nM	CHEMBL3311301
8.08	EC50	8.4	nM	CHEMBL6001886
8.06	EC50	8.8	nM	CHEMBL5964486
8.05	EC50	9	nM	CHEMBL4743917
8.04	EC50	9.1	nM	CHEMBL2336646
8.00	EC50	10	nM	CHEMBL5556797
8.00	EC50	10	nM	CHEMBL5186339
8.00	EC50	10	nM	CHEMBL5208504
8.00	EC50	10	nM	N-FORMYLMETHIONYL-LEUCYLPHENYLALANINE

PubChem BioAssay actives

539 with measured affinity, of 1244 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
1-(6-chloro-1,2,3,4-tetrahydronaphthalen-2-yl)-3-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-(4-methoxy-1-methyl-2-oxo-3-pyridinyl)-2-oxopyrrolidin-3-yl]urea	2083658: Agonist activity at FPR1 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0005	uM
(2S)-2-[[2-[(4-bromophenyl)carbamoylamino]acetyl]amino]-4-methylpentanoic acid	1932192: Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay	ec50	0.0006	uM
(2S)-4-methyl-2-[[2-[[4-(trifluoromethyl)phenyl]carbamoylamino]acetyl]amino]pentanoic acid	2083647: Agonist activity at human FPR1 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-4 AM dye based fluorescence assay	ec50	0.0006	uM
1-[(3R)-1-[4-[2-(tert-butylsulfamoyl)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-(4-chlorophenyl)urea	2083658: Agonist activity at FPR1 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0006	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[(4-chlorophenyl)carbamoylamino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	91146: Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils	ec50	0.0010	uM
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-methoxyphenyl)-2-oxopiperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-chlorophenyl)-3-[(3R,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-(3,3-difluoropropyl)piperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-chlorophenyl)-3-[(3R,4R)-1-(cyclopropylmethyl)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopiperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-fluorophenyl)-3-[(3R,4S)-4-(4-methoxyphenyl)-2-oxo-1-(pyridin-2-ylmethyl)piperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-fluorophenyl)-3-[(3R,4R)-4-(4-methoxyphenyl)-2-oxo-1-(pyridin-2-ylmethyl)piperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-fluorophenyl)-3-[(3R,4R)-4-(4-methoxyphenyl)-2-oxo-1-(pyridin-3-ylmethyl)piperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
1-(4-chlorophenyl)-3-[(3R,4R)-4-(4-methoxyphenyl)-1-pyridazin-4-ylpiperidin-3-yl]urea	1932236: Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay	ec50	0.0010	uM
2-[[(2S)-2-[[(2S)-2-[(4-methoxyphenyl)carbamoylamino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	91146: Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils	ec50	0.0010	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[2-[ethoxy(methyl)phosphoryl]phenyl]-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	2083658: Agonist activity at FPR1 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0011	uM
2-[1-[(4-bromophenyl)carbamoylamino]ethyl]-3-methylbutanoic acid	1932192: Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay	ec50	0.0017	uM
(2S)-2-[[(2S)-4-methyl-2-[[(2S)-2-[(4-methylphenyl)carbamoylamino]-4-methylsulfanylbutanoyl]amino]pentanoyl]amino]-3-phenylpropanoic acid	219067: Binding affinity towards fMLF receptor using human neutrophils	ic50	0.0020	uM
methyl 3-[4-[[4-(difluoromethoxy)benzoyl]amino]-3-(2,6-difluoro-4-methoxyphenyl)-2-methyl-5-oxopyrazol-1-yl]benzoate	2083654: Agonist activity at human FPR1 transfected in CHO cells by cAMP assay	ec50	0.0020	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-3-(4-benzoylphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-4-methylpentanoyl]amino]-3-(cyclohexen-1-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	1184057: Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of intracellular calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method	kd	0.0021	uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoate	730964: Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as induction of chemotaxis after 60 mins	ec50	0.0025	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-phenylurea	1932223: Agonist activity at human FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay	ec50	0.0028	uM
4-(difluoromethoxy)-N-[3-(2,6-difluoro-4-methoxyphenyl)-1-[3-(difluoromethoxy)phenyl]-2-methyl-5-oxopyrazol-4-yl]benzamide	2083654: Agonist activity at human FPR1 transfected in CHO cells by cAMP assay	ec50	0.0030	uM
4-(difluoromethoxy)-N-[3-(2,6-difluoro-4-methoxyphenyl)-1-(3-methoxyphenyl)-2-methyl-5-oxopyrazol-4-yl]benzamide	2083654: Agonist activity at human FPR1 transfected in CHO cells by cAMP assay	ec50	0.0030	uM
(2S)-2-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	1196961: Binding affinity to human FPR1 receptor	kd	0.0030	uM
1-(4-chlorophenyl)-3-[(3S,4R)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720304: Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method	ec50	0.0039	uM
N-[(2S)-3,3-dimethylbutan-2-yl]-1-(4-methoxycyclohexyl)-3-methyl-5-[(4-methylphenyl)sulfonylamino]pyrazole-4-carboxamide	638993: Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay	ic50	0.0040	uM
trans-methyl (1R,2S)-1-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-2-phenylcyclopropane-1-carboxylate	730964: Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as induction of chemotaxis after 60 mins	ec50	0.0047	uM
(2S)-2-[[2-[(4-bromophenyl)carbamoylamino]acetyl]amino]pentanoic acid	1932192: Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay	ec50	0.0049	uM
4-(difluoromethoxy)-N-[5-(2,6-difluoro-4-methoxyphenyl)-1-methyl-2-[6-(3-methylpyrazol-1-yl)-2-pyridinyl]-3-oxopyrazol-4-yl]benzamide	2083654: Agonist activity at human FPR1 transfected in CHO cells by cAMP assay	ec50	0.0050	uM
N-(4-bromophenyl)-2-[5-[(2,3-dimethoxyphenyl)methyl]-3-methyl-6-oxopyridazin-1-yl]hexanamide	1555095: Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay	ec50	0.0065	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-3-(4-benzoylphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-4-methylpentanoyl]amino]-3-(cyclohexen-1-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-cyclohexylpropanoic acid	1184057: Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of intracellular calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method	kd	0.0069	uM
1-(4-fluorophenyl)-3-[(3S,4R)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720304: Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method	ec50	0.0090	uM
cis-(1R,2R)-1-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-2-phenylcyclopropane-1-carboxylic acid	730964: Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as induction of chemotaxis after 60 mins	ec50	0.0091	uM
1-(4-chlorophenyl)-3-[(3S,4S)-4-(4-methoxyphenyl)-2-oxopiperidin-3-yl]urea	1720304: Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method	ec50	0.0100	uM
4-(difluoromethoxy)-N-[3-(2,6-difluoro-4-methoxyphenyl)-1-(3,5-dimethoxyphenyl)-2-methyl-5-oxopyrazol-4-yl]benzamide	2083654: Agonist activity at human FPR1 transfected in CHO cells by cAMP assay	ec50	0.0100	uM
(3S,4R)-3-(1H-benzimidazol-2-ylamino)-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one	2083660: Agonist activity at FPR1 (unknown origin) transfected in CHO cells by cAMP assay	ec50	0.0100	uM
(3R,4R)-3-(1H-benzimidazol-2-yl)-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one	2083660: Agonist activity at FPR1 (unknown origin) transfected in CHO cells by cAMP assay	ec50	0.0100	uM
1-[(3R)-2-oxo-1-(4-piperidin-1-ylphenyl)piperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	1932217: Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay	ec50	0.0110	uM
N-[(2S)-3,3-dimethylbutan-2-yl]-1-(4-fluorophenyl)-3-methyl-5-[[4-(trifluoromethyl)phenyl]sulfonylamino]pyrazole-4-carboxamide	630742: Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay	ic50	0.0126	uM
trans-methyl (1S,2R)-1-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-2-phenylcyclopropane-1-carboxylate	730964: Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as induction of chemotaxis after 60 mins	ec50	0.0140	uM
(2S)-2-[[2-[(4-bromophenyl)carbamoylamino]acetyl]amino]-3-phenylpropanoic acid	1932192: Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay	ec50	0.0147	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-3-(4-benzoylphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	1184057: Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of intracellular calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method	kd	0.0160	uM
1-[(3S,4R)-4-(2,5-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1720304: Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method	ec50	0.0170	uM
N-(4-bromophenyl)-2-[5-[(3-methoxyphenyl)methyl]-3,4-dimethyl-6-oxopyridazin-1-yl]acetamide	1932202: Agonist activity at human FPR1 transfected in HL-60 cells assessed as increase in intracellular calcium flux incubated for 30 mins by Fluo-4 AM dye based FLIPR-fluorometeric assay	ec50	0.0190	uM
(2S)-2-[[(2R)-4-methyl-2-[[(2S)-2-[[(2R)-4-methyl-2-[[(2S)-2-[(3-methylphenyl)carbamoylamino]-3-phenylpropanoyl]amino]pentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]amino]-3-phenylpropanoic acid	91150: Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils	ic50	0.0200	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphoryl-3-fluorophenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	2083658: Agonist activity at FPR1 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0200	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-(1-adamantylcarbamoylamino)-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	219067: Binding affinity towards fMLF receptor using human neutrophils	ic50	0.0200	uM
cis-methyl (1S,2S)-1-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-2-phenylcyclopropane-1-carboxylate	730964: Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as induction of chemotaxis after 60 mins	ec50	0.0210	uM
(2R)-3-(1H-indol-3-yl)-N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-2-[(4-nitrophenyl)carbamoylamino]propanamide	2083642: Agonist activity at human FPR1 expressed in HL-60 cells assessed as increase in calcium mobilization by FLIPR analysis	ec50	0.0230	uM
(2S)-2-[[(2R)-2-[[(2S)-3-cyclohexyl-2-[[(2R)-4-methyl-2-[[(2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]amino]pentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid	1184057: Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of intracellular calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method	kd	0.0250	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	2083658: Agonist activity at FPR1 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0250	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Air Pollutants	decreases expression, affects expression, increases abundance	3
Nickel	decreases expression, increases expression	3
Calcitriol	decreases expression, increases expression, affects cotreatment	2
Dexamethasone	affects binding, decreases reaction, increases expression	2
Methotrexate	decreases expression	2
Particulate Matter	decreases expression, increases abundance, increases expression	2
alpha phellandrene	decreases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
sulforaphane	increases expression	1
cobaltous chloride	increases expression	1
butyraldehyde	increases expression	1
tetrathiomolybdate	increases expression	1
pentanal	increases expression	1
di-n-butylphosphoric acid	affects expression	1
Trp-Lys-Tyr-Met-Val-Met	affects binding, decreases reaction, increases activity	1
nordy	decreases expression	1
Grape Seed Proanthocyanidins	decreases expression	1
(+)-JQ1 compound	decreases expression	1
Pioglitazone	decreases expression	1
Decitabine	affects binding, increases reaction, decreases expression	1
Arsenic Trioxide	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants, Occupational	decreases expression	1
Aldehydes	increases expression	1
Aspirin	decreases expression	1
Benzene	increases expression	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Endosulfan	increases expression	1
N-Formylmethionine Leucyl-Phenylalanine	affects binding, increases activity	1

ChEMBL screening assays

138 unique, capped per target: 85 functional, 53 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2342907	Binding	Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as stimulation of fMLP-OMe-induced superoxide radical generation at 0.1 uM incubated for 5 mins followed by fMLP-OMe induction by spectrophotometric analysis relative to c	A formyl peptide substituted with a conformationally constrained phenylalanine residue evokes a selective immune response in human neutrophils. — Bioorg Med Chem
CHEMBL2342908	Functional	Agonist activity at FPR1/FPR2 receptor in human neutrophils assessed as increase in intracellular calcium concentration by spectrofluorophotometric analysis	A formyl peptide substituted with a conformationally constrained phenylalanine residue evokes a selective immune response in human neutrophils. — Bioorg Med Chem

Cellosaurus cell lines

5 cell lines: 3 spontaneously immortalized cell line, 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_E4JG	L1-2 FPR	Cancer cell line
CVCL_H431	CHO-K1/FPR1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV15	cAMP Hunter CHO-K1 FPR1 Gi	Spontaneously immortalized cell line	Female
CVCL_KX05	PathHunter CHO-K1 FPR1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA31	PathHunter U2OS FPR1 Total GPCR Internalization	Cancer cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00152750	PHASE4	UNKNOWN	Study of Clonidine on Sleep Architecture in Children With Tourette’s Syndrome (TS) and Comorbid ADHD
NCT00226824	PHASE4	TERMINATED	Safety Study of Galantamine in Tic Disorders
NCT00241176	PHASE4	COMPLETED	Open Label Trial of Aripiprazole in Children and Adolescents With Tourette’s Disorder
NCT00370838	PHASE4	COMPLETED	Comparison of Keppra and Clonidine in the Treatment of Tics
NCT01018056	PHASE4	COMPLETED	Developing New Treatments for Tourette Syndrome: Therapeutic Trials With Modulators of Glutamatergic Neurotransmission
NCT01547000	PHASE4	COMPLETED	Guanfacine in Children With Tic Disorders
NCT03239210	PHASE4	COMPLETED	Effects of Ondansetron in Obsessive-compulsive and Tic Disorders
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	PHASE4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	PHASE4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	PHASE4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	PHASE4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	PHASE4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	PHASE4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	PHASE4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	PHASE4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	PHASE4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	PHASE4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	PHASE4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	PHASE4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	PHASE4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	PHASE4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	PHASE4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	PHASE4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	PHASE4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	PHASE4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	PHASE4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	PHASE4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	PHASE4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	PHASE4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	PHASE4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	PHASE4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	PHASE4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	PHASE4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	PHASE4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	PHASE4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	PHASE4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	PHASE4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	PHASE4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	PHASE4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy