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): 271 total
• GTEx eGene: eQTL in 34 tissues, sQTL in 4 (q < 0.05)
• ChEMBL bioactivity: 11 clinical-phase molecules tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.13 (intermediate), LOEUF 1.92 (unconstrained)
• MANE Select transcript: NM_002029
• Notable: 271 clinical variants but no curated precision-oncology (CIViC) evidence yet

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: 16 — 16 protein_coding

MANE Select: ENST00000304748

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1, TSL 2: 1, TSL 3: 1, TSL 4: 1

ENST00000304748, ENST00000594900, ENST00000595042, ENST00000600815, ENST00000881808, ENST00000881809, ENST00000881810, ENST00000930484, ENST00000948394, ENST00000948395, ENST00000948396, ENST00001095018, ENST00001095019, ENST00001126873, ENST00001126874, ENST00001136045

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.

Highest expression (Bgee): blood, monocyte, leukocyte, mononuclear cell, periodontal ligament.

Genetic regulation across tissues (GTEx eQTL / sQTL)

FPR1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 34 tissues and its splicing (sQTL) in 4 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 38 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Whole Blood	sqtl	8.3e-49	-0.50	19:51751098:T:C
Cells Cultured fibroblasts	eqtl	3.7e-41	+0.91	19:51741925:G:A
Nerve Tibial	eqtl	1.1e-39	+0.35	19:51751943:A:G
Skin Sun Exposed Lower leg	eqtl	1.1e-20	+0.32	19:51753248:A:G
Lung	sqtl	1.3e-20	-0.47	19:51752736:A:C
Whole Blood	eqtl	4.9e-19	+0.12	19:51755288:C:T
Adipose Subcutaneous	eqtl	2.0e-17	+0.23	19:51751943:A:G
Artery Tibial	eqtl	1.5e-15	+0.24	19:51751943:A:G
Lung	eqtl	4.6e-13	+0.18	19:51755288:C:T
Colon Sigmoid	eqtl	2.4e-11	+0.26	19:51751943:A:G
Breast Mammary Tissue	eqtl	2.6e-11	+0.23	19:51751943:A:G
Skin Not Sun Exposed Suprapubic	eqtl	2.0e-10	+0.27	19:51751943:A:G
Artery Aorta	eqtl	2.7e-10	+0.19	19:51751943:A:G
Brain Caudate basal ganglia	eqtl	4.3e-10	+0.26	19:51751943:A:G
Thyroid	eqtl	9.5e-10	+0.23	19:51753248:A:G
Esophagus Muscularis	eqtl	2.0e-09	+0.18	19:51751943:A:G
Adrenal Gland	eqtl	2.0e-09	+0.29	19:51755312:C:T
Colon Transverse	eqtl	2.8e-09	+0.23	19:51747508:A:G
Adipose Visceral Omentum	eqtl	3.9e-09	+0.13	19:51755312:C:T
Pancreas	eqtl	8.3e-08	+0.27	19:51755312:C:T

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

showing 100 of 279 tissues 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
left adrenal gland	UBERON:0001234	81.36	gold quality
left adrenal gland cortex	UBERON:0035825	81.04	gold quality
spinal cord	UBERON:0002240	80.96	gold quality
caecum	UBERON:0001153	80.85	gold quality
pericardium	UBERON:0002407	80.83	gold quality
palpebral conjunctiva	UBERON:0001812	80.33	gold quality
right adrenal gland	UBERON:0001233	79.63	gold quality
mucosa of stomach	UBERON:0001199	79.53	gold quality
smooth muscle tissue	UBERON:0001135	79.43	gold quality
aorta	UBERON:0000947	79.34	gold quality
lymph node	UBERON:0000029	79.11	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	79.00	gold quality
placenta	UBERON:0001987	78.92	gold quality
hindlimb stylopod muscle	UBERON:0004252	78.26	gold quality
eye	UBERON:0000970	78.20	gold quality
right atrium auricular region	UBERON:0006631	77.97	gold quality
pancreatic ductal cell	CL:0002079	77.77	silver quality
adrenal cortex	UBERON:0001235	77.76	gold quality
subcutaneous adipose tissue	UBERON:0002190	77.52	gold quality
right adrenal gland cortex	UBERON:0035827	77.34	gold quality
heart left ventricle	UBERON:0002084	76.81	gold quality
adrenal gland	UBERON:0002369	76.81	gold quality
tibial artery	UBERON:0007610	76.58	gold quality
popliteal artery	UBERON:0002250	76.53	gold quality
cardiac ventricle	UBERON:0002082	76.46	gold quality
tibial nerve	UBERON:0001323	76.00	gold quality
heart right ventricle	UBERON:0002080	75.96	gold quality
apex of heart	UBERON:0002098	75.87	gold quality
heart	UBERON:0000948	75.83	gold quality
cardiac atrium	UBERON:0002081	75.64	gold quality
adipose tissue	UBERON:0001013	75.47	gold quality
right lobe of liver	UBERON:0001114	75.25	gold quality
liver	UBERON:0002107	74.94	gold quality
connective tissue	UBERON:0002384	74.92	gold quality
superficial temporal artery	UBERON:0001614	74.15	silver quality
right lobe of thyroid gland	UBERON:0001119	73.88	gold quality
substantia nigra	UBERON:0002038	73.50	gold quality
endometrium epithelium	UBERON:0004811	72.72	silver quality
lower esophagus muscularis layer	UBERON:0035833	72.72	gold quality
lower esophagus	UBERON:0013473	72.67	gold quality
muscle layer of sigmoid colon	UBERON:0035805	72.60	gold quality
endocervix	UBERON:0000458	72.46	gold quality
body of stomach	UBERON:0001161	72.13	gold quality
gastrocnemius	UBERON:0001388	72.09	gold quality
hypothalamus	UBERON:0001898	71.96	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	71.96	gold quality
minor salivary gland	UBERON:0001830	71.66	gold quality
right ovary	UBERON:0002118	71.62	gold quality
midbrain	UBERON:0001891	71.57	gold quality
urinary bladder	UBERON:0001255	71.53	gold quality
cauda epididymis	UBERON:0004360	71.33	gold quality
anatomical system	UBERON:0000467	70.86	gold quality
caudate nucleus	UBERON:0001873	70.80	gold quality
parietal pleura	UBERON:0002400	70.70	silver quality
multicellular organism	UBERON:0000468	70.66	gold quality
material anatomical entity	UBERON:0000465	70.63	gold quality
left lobe of thyroid gland	UBERON:0001120	70.58	gold quality
amygdala	UBERON:0001876	70.48	gold quality
pigmented layer of retina	UBERON:0001782	70.46	silver quality
retina	UBERON:0000966	70.45	silver quality
pleura	UBERON:0000977	70.21	silver quality
transverse colon	UBERON:0001157	70.12	gold quality
nasal cavity epithelium	UBERON:0005384	70.04	silver quality
small intestine Peyer’s patch	UBERON:0003454	69.96	gold quality
esophagus	UBERON:0001043	69.82	gold quality
body of pancreas	UBERON:0001150	69.80	gold quality
muscle of leg	UBERON:0001383	69.56	gold quality
rectum	UBERON:0001052	69.47	gold quality
buccal mucosa cell	CL:0002336	69.46	silver quality
caput epididymis	UBERON:0004358	69.10	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

HPA expression

RNA tissue specificity: Tissue enhanced

53 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Bone marrow	tissue	179.3	medium
Appendix	tissue	153.9	low
Spleen	tissue	67.4	low
Adipose tissue	tissue	63.7	not detected
Urinary bladder	tissue	62.0	not detected
Placenta	tissue	41.7	not detected
Smooth muscle	tissue	38.9	not detected
Lung	tissue	28.1	low
Medulla oblongata	tissue	27.3
Gallbladder	tissue	25.9	not detected
Tongue	tissue	20.6
Liver	tissue	19.5	not detected
Spinal cord	tissue	16.2
Lymph node	tissue	11.6	low
Choroid plexus	tissue	10.8
Pancreas	tissue	9.8	not detected
Tonsil	tissue	9.4	low
Adrenal gland	tissue	9.2	not detected
Substantia nigra	tissue	8.8
Retrosplenial cortex	tissue	8.4
Esophagus	tissue	8.2	not detected
Thymus	tissue	7.8
Cervix	tissue	7.6	not detected
Locus coeruleus	tissue	7.6
Putamen	tissue	6.3
Nucleus accumbens	tissue	6.3
Hippocampus	tissue	6.2	not detected
Fallopian tube	tissue	6.1	not detected
Parathyroid gland	tissue	4.7	not detected
Pituitary gland	tissue	4.6
Small intestine	tissue	4.6	low
Breast	tissue	4.4	not detected
Colon	tissue	4.2	low
Kidney	tissue	3.6	not detected
Vagina	tissue	3.5	not detected
Stomach 1	tissue	3.1	low
Rectum	tissue	2.9	low
Duodenum	tissue	2.8	not detected
Thyroid gland	tissue	2.6	not detected
Prostate	tissue	2.5	not detected
Postcentral gyrus	tissue	2.5
Heart muscle	tissue	2.4	low
Salivary gland	tissue	2.2	not detected
Seminal vesicle	tissue	2.0	not detected
Testis	tissue	1.6	low
Endometrium 1	tissue	1.6	not detected
Retina	tissue	1.5
Ovary	tissue	1.3	not detected
Skeletal muscle	tissue	0.7	low
Epididymis	tissue	0.5	low
Skin 1	tissue	0.4	not detected
Cerebral cortex	tissue	0.1	not detected
Occipital cortex	tissue	0.1

Brain sub-regions (HPA Brain Atlas): detected in 185; highest nTPM — Lateral funiculus (white matter) (31.9), Nucleus raphe pallidus (27.3), Medial olivary nucleus (19.8), Anterior funiculus (white matter) (18.7), Peritrigeminal nucleus (17.6).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): IRF6, SPI1

miRNA regulators (miRDB)

Targeting FPR1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

11 miRNAs:

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

Functional genomics

gnomAD constraint: pLI 0.132, LOEUF 1.92, missense Z 1.16 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000304748 — one region, missense o/e 0.90.

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)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:107443) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 4 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased susceptibility to bacterial infection	1
abnormal innate immunity	1
impaired neutrophil chemotaxis	1
increased susceptibility to bacterial infection induced morbidity/mortality	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan paniscus	Q49SQ2	99.7%	Diamond
Pan troglodytes	Q49SQ3	99.7%	Diamond
Sus scrofa	P79291	99.6%	Diamond
Macaca mulatta	O97664	99.2%	Diamond
Macaca fascicularis	Q95LH1	99.2%	Diamond
Cavia porcellus	P97266	99.0%	Diamond
Gorilla gorilla gorilla	P79177	98.9%	Diamond
Pongo pygmaeus	P79234	97.9%	Diamond
Cricetulus longicaudatus	Q00991	89.5%	Diamond
Rattus rattus	Q49SP8	89.4%	Diamond
Bos taurus	B9VR26	85.4%	Diamond
Oryctolagus cuniculus	Q05394	79.2%	Diamond
Canis lupus familiaris	P30992	69.8%	Diamond
Danio rerio	P0C7U5	59.5%	Diamond
Oncorhynchus mykiss	Q6UNA4	59.5%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
FPR2	protein-coding	2358
FPR3	protein-coding	2359
ZNF577	protein-coding	84765
SPACA6-AS1	ncRNA	102238594
SPACA6	protein-coding	147650
HAS1	protein-coding	3036
MIR125A	ncRNA	406910
MIRLET7E	ncRNA	406887
MIR99B	ncRNA	407056

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 (81 total): mutagenesis site 16, helix 15, 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 by resolution:

PDB	Title	Method	Resolution (Å)
7VFX	The structure of Formyl Peptide Receptor 1 in complex with Gi and peptide agonist fMIFL	ELECTRON MICROSCOPY	2.8
7EUO	The structure of formyl peptide receptor 1 in complex with Gi and peptide agonist fMLF	ELECTRON MICROSCOPY	2.9
9KFT	Cryo-EM structure of the fMLFC-FPR1-Gi complex	ELECTRON MICROSCOPY	3.06
7T6T	Structure of the human FPR1-Gi complex with fMLFII	ELECTRON MICROSCOPY	3.2
7WVU	Cryo-EM structure of the human formyl peptide receptor 1 in complex with fMLF and Gi1	ELECTRON MICROSCOPY	3.3

Predicted structure (AlphaFold)

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

Antibody-complex structures (SAbDab)

3 antibodies co-crystallized with this protein: 7EUO, 7VFX, 9KFT

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Chemokines and chemotactic factors receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): golgi apparatus; nucleoli; nucleoplasm

Antibody reliability (HPA): IH approved · IF approved

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)

Position	Role
106	N(alpha)-formyl-L-methionyl-L-isoleucyl-L-phenylalanyl-L-leucine
106	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-isoleucine
201	N(alpha)-formyl-L-methionyl-L-isoleucyl-L-phenylalanyl-L-leucine
201	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanine
201	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-isoleucine
205	N(alpha)-formyl-L-methionyl-L-isoleucyl-L-phenylalanyl-L-leucine
205	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanine
205	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-isoleucine
257	N(alpha)-formyl-L-methionyl-L-isoleucyl-L-phenylalanyl-L-leucine
257	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanine
257	N(alpha)-formyl-L-methionyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-isoleucine

Post-translational modifications (8)

Type	Positions
Phosphoserine	328, 332, 338
Phosphothreonine	329, 331, 334, 336, 339

Disulfide bonds (1)

Type	Positions
Disulfide bond	98–176

Glycosylation sites (2)

Type	Positions
N-linked (glcnac…) asparagine	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 agonist potency of …
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 potency of …
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 peptides fmifl and …
205	abolishes the response to n-formyl peptide fmlf. decreases intracellular camp reduction upon stimulation with n-formyl peptides fmifl and …
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 curated (TAS) of 14; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

14 pathways:

ID	Pathway	Evidence
R-HSA-444473	Formyl peptide receptors bind formyl peptides and many other ligands	curated
R-HSA-418594	G alpha (i) signalling events	curated
R-HSA-6783783	Interleukin-10 signaling	curated
R-HSA-6798695	Neutrophil degranulation	curated
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-1280215	Cytokine Signaling in Immune system	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-168256	Immune System	—
R-HSA-168249	Innate Immune System	—
R-HSA-375276	Peptide ligand-binding receptors	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—
R-HSA-449147	Signaling by Interleukins	—

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 (12): 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), innate immune response (GO:0045087), immune system process (GO:0002376), 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

10 top-level categories:

Category	Pathways
Immune System	2
Signaling by GPCR	2
GPCR downstream signalling	1
Peptide ligand-binding receptors	1
Signaling by Interleukins	1
Innate Immune System	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1
Cytokine Signaling in Immune system	1

GO top-level categories

38 GO namespaces:

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
immune response	1
defense response to symbiont	1
biological_process	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

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 4 of 26 annotations. The rest are phylogenetic / computational / electronic (IEA).

4 experimentally-supported GO terms:

GO term	NS	Evidence
phospholipase C-activating G protein-coupled receptor signaling pathway	BP	direct assay
G protein-coupled receptor activity	MF	direct assay
G protein-coupled receptor binding	MF	direct assay
N-formyl peptide receptor activity	MF	direct assay

Protein interactions and networks

STRING

showing 16 of 1,624 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FPR1	ANXA1	P04083	900
FPR1	RPTOR	Q8N122	742
FPR1	TREM1	Q9NP99	684
FPR1	TLR4	O00206	647
FPR1	MLST8	Q9BVC4	635
FPR1	KHDRBS2	Q5VWX1	630
FPR1	KHDRBS3	O75525	630
FPR1	TREM2	Q9NZC2	608
FPR1	TLR9	Q9NR96	606
FPR1	TLR8	Q9NR97	510
FPR1	KIR2DL1	P43626	501
FPR1	IFNGR1	P15260	484
FPR1	RARRES2	Q99969	444
FPR1	IL1B	P01584	441
FPR1	CAMP	P49913	441
FPR1	CXCL8	P10145	441

IntAct

Human interaction partners of FPR1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

9 partners by confidence:

Partner	Interaction type	MIscore	Records
MAPK13	physical association	0.500	3
GRK2	physical association	0.500	2
MAPK3	physical association	0.400	1
RAMP1	physical association	0.400	1
RAMP2	physical association	0.400	1
RAMP3	physical association	0.400	1
GPR89A	association	0.350	1
NBAS	association	0.350	1
RAB29	association	0.350	1

BioGRID (143 interactions; top human partners by supporting records): AARS2 (Affinity Capture-MS), ABCB8 (Affinity Capture-MS), ACTB (Co-fractionation), ADCK1 (Affinity Capture-MS), ADCK4 (Affinity Capture-MS), AGER (Affinity Capture-Western), AMFR (Affinity Capture-MS), ANKRD44 (Affinity Capture-MS), ANXA1 (Affinity Capture-Western), AP5Z1 (Affinity Capture-MS), ARFGEF1 (Affinity Capture-MS), ARFGEF2 (Affinity Capture-MS), ATL2 (Affinity Capture-MS), ATL3 (Affinity Capture-MS), ATM (Affinity Capture-MS)

SIGNOR signaling

showing 6 of 12 signaling 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

Ligand–receptor pairs (CellPhoneDB) (3)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

3 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
CTSG	receptor	Signaling by Cathepsin
TAFA4	receptor	Signaling by TAFA
ANXA1	receptor	Signaling by Annexin

Disease & clinical

Genetic variants

Variant evidence for FPR1: 271 ClinVar records (0 pathogenic / likely pathogenic); 8 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	158
Likely benign	90
Benign	16

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 17 predictions of 192):

Position(s)	Effect	Δscore	Sites
19:51751813	donor_loss	1.0000	2
19:51747006–51747007	acceptor_loss	0.9900	6
19:51751812	donor_loss	0.9900	2
19:51751813	donor_loss	0.9800
19:51747014	acceptor_gain	0.9000
19:51747005	acceptor_gain	0.8800
19:51747008	acceptor_loss	0.8100
19:51747018	acceptor_gain	0.8100
19:51751129	donor_gain	0.7700
19:51746969	acceptor_gain	0.7100

AlphaMissense

707 missense substitutions predicted likely pathogenic (of 2,286 scored), across 214 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
N44	8	0.948	0.982
D71	8	0.943	0.983
D106	8	0.901	0.951
F250	8	0.894	0.992
D122	8	0.893	0.947
N297	8	0.880	0.964
F74	8	0.822	0.960
C176	7	0.977	0.988
W91	7	0.971	0.994
C98	7	0.971	0.986
F210	7	0.947	0.992
F110	7	0.928	0.977
W254	7	0.914	0.972
F180	7	0.911	0.969
F93	7	0.888	0.913
W150	7	0.852	0.971
F178	7	0.830	0.931
F206	7	0.824	0.943
F308	7	0.816	0.949
F114	7	0.808	0.908

HPA cancer prognostics

RNA cancer specificity: Cancer enhanced (Glioblastoma Multiforme)

Disease associations

OMIM: gene MIM:136537 | disease phenotypes:

GenCC curated gene-disease

2 curated gene-disease records:

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

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (2 panels, 1 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

2 panels:

Panel	Rating
COVID-19 research	green
Primary immunodeficiency or monogenic inflammatory bowel disease	amber

Mondo (2): Tourette syndrome (MONDO:0007661), susceptibility to localized juvenile periodontitis (MONDO:0018643)

GWAS associations

8 associations:

Study	Trait	p-value
GCST90002382_444	Eosinophil percentage of white cells	1e-18
GCST90002381_205	Eosinophil count	3e-18
GCST90002388_106	Lymphocyte count	5e-10
GCST90002399_181	Neutrophil percentage of white cells	8e-10
GCST004623_4	Neutrophil percentage of granulocytes	7e-9
GCST010796_2706	Electrocardiogram morphology (amplitude at temporal datapoints)	1e-8
GCST007277_24	Tourette syndrome	9e-7
GCST004866_7	Alopecia areata	6e-6

EFO canonical traits (from GWAS)

6 canonical traits:

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

1 disease descriptors:

Descriptor	Name	Tree numbers
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

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 194,291 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

11 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1471	APREPITANT	4	935
CHEMBL1200776	CINACALCET HYDROCHLORIDE	4	1,229
CHEMBL1707	LOPERAMIDE HYDROCHLORIDE	4	59,642
CHEMBL1200681	MONTELUKAST SODIUM	4	10,986
CHEMBL1223	PENICILLIN G POTASSIUM	4	20,711
CHEMBL567	PERPHENAZINE	4	22,063
CHEMBL101	PHENYLBUTAZONE	4	59,810
CHEMBL832	SULFINPYRAZONE	4	13,851
CHEMBL1230609	FORETINIB	2	3,230
CHEMBL405355	NIGULDIPINE	2	1,809
CHEMBL4784510	BMS-986235	1	25

PharmGKB: 1 entry (CPIC guideline: no)

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)

1386 measured of 1791 human assays (1815 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
CHEMBL4776349	EC50	0.05 nM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphoryl-3-fluorophenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.077 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
CHEMBL4743917	EC50	0.085 nM
CHEMBL4755590	EC50	0.087 nM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-(4-methoxy-1-methyl-2-oxo-3-pyridinyl)-2-oxopyrrolidin-3-yl]-3-phenylurea	EC50	0.1 nM	US-20230303513: OXOPYRROLIDINE UREA FPR2 AGONISTS
4-chloro-N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-[1-(2-hydroxypropyl)-4-methyl-2-oxo-3-pyridinyl]-2-oxopyrrolidin-3-yl]benzamide	EC50	0.1 nM	US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS
CHEMBL4784400	EC50	0.11 nM
CHEMBL4758920	EC50	0.11 nM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	EC50	0.13 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-(4-chlorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	EC50	0.14 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
CHEMBL4744835	EC50	0.15 nM
1-[(3R)-1-[3-fluoro-4-[1-(methanesulfonamidomethyl)cyclopropyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	EC50	0.17 nM	US-11124494: Aryl heterocyclic piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R,5R)-5-hydroxy-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	EC50	0.17 nM	US-11186544: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-[(3R)-1-[4-[3-(dimethylamino)piperidin-1-yl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	EC50	0.18 nM	US-11008301: Piperidinone formyl peptide 2 receptor agonists
CHEMBL4744094	EC50	0.18 nM
CHEMBL4761554	EC50	0.19 nM
1-(6-chloro-1,2,3,4-tetrahydronaphthalen-2-yl)-3-[(3S,4R)-1-[1-(2-methoxyethyl)-2-oxo-3-pyridinyl]-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	EC50	0.2 nM	US-20230303513: OXOPYRROLIDINE UREA FPR2 AGONISTS
4-(difluoromethoxy)-N-[(3S,4S,5S)-4-(2,6-difluoro-4-methoxyphenyl)-5-methyl-2-oxo-1-(6-piperidin-4-yl-2-pyridinyl)pyrrolidin-3-yl]benzamide	EC50	0.2 nM	US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS
1-[(3R)-1-[4-[1-(methanesulfonamidomethyl)cyclopropyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	EC50	0.21 nM	US-11124494: Aryl heterocyclic piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R,5S)-1-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-5-(methoxymethyl)-2-oxopyrrolidin-3-yl]urea	EC50	0.22 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R,5S)-1-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-5-(hydroxymethyl)-2-oxopyrrolidin-3-yl]urea	EC50	0.27 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-(4-methoxyphenyl)urea	EC50	0.28 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphoryl-3-pyridinyl)-2,3-difluorophenyl]-5-methyl-2-oxopyrrolidin-3-yl]urea	EC50	0.3 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[3-(dimethylamino)pyrrolidin-1-yl]-2-fluorophenyl]-2-oxopiperidin-3-yl]urea	EC50	0.31 nM	US-11008301: Piperidinone formyl peptide 2 receptor agonists
1-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	EC50	0.32 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
CHEMBL4778725	EC50	0.32 nM
2-(3-chlorophenyl)-4-N-methyltriazole-4,5-diamine	EC50	0.325 nM
1-(4-chlorophenyl)-3-[(3R,5R)-5-hydroxy-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	EC50	0.35 nM	US-11186544: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-[(3R)-1-[4-[2-[methyl(methylsulfonyl)amino]-3-pyridinyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	EC50	0.36 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
CHEMBL4753713	EC50	0.36 nM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphoryl-3-pyridinyl)-2,3-difluorophenyl]-4,4-dimethyl-2-oxopyrrolidin-3-yl]urea	EC50	0.39 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chlorophenyl)-3-[(3R)-1-[4-[3-(dimethylamino)pyrrolidin-1-yl]-3-fluorophenyl]-2-oxopiperidin-3-yl]urea	EC50	0.39 nM	US-11008301: Piperidinone formyl peptide 2 receptor agonists
1-(6-chloro-1,2,3,4-tetrahydronaphthalen-2-yl)-3-[(3S,4R)-1-(1-ethyl-2-oxo-3-pyridinyl)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	EC50	0.4 nM	US-20230303513: OXOPYRROLIDINE UREA FPR2 AGONISTS
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-[4-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]-3-(trifluoromethyl)-2-pyridinyl]-2-oxopyrrolidin-3-yl]-3-[4-(difluoromethyl)cyclohexyl]urea	EC50	0.4 nM	US-20230303513: OXOPYRROLIDINE UREA FPR2 AGONISTS
N-[(3S,4R)-1-[1-(2,2-difluoroethyl)-4-methyl-2-oxo-3-pyridinyl]-4-(2-fluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-4-(difluoromethoxy)benzamide	EC50	0.4 nM	US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphorylphenyl)-2-fluoro-3-(trifluoromethyl)phenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.41 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chlorophenyl)-3-[(3R)-1-[2,3-difluoro-4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.43 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-5-methyl-2-oxopyrrolidin-3-yl]urea	EC50	0.44 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
CHEMBL4745044	EC50	0.45 nM
1-[(3R)-1-[4-[2-(tert-butylsulfamoyl)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-(4-chlorophenyl)urea	EC50	0.46 nM	US-10717708: Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(7R)-5-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-6-oxo-5-azaspiro[2.4]heptan-7-yl]urea	EC50	0.48 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]-2-propan-2-ylphenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.5 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-[1-(2-methoxyethyl)-4-methyl-2-oxo-3-pyridinyl]-2-oxopyrrolidin-3-yl]-3-(6-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)urea	EC50	0.5 nM	US-20230303513: OXOPYRROLIDINE UREA FPR2 AGONISTS
4-chloro-N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-(3-methoxy-2-pyridinyl)-2-oxopyrrolidin-3-yl]benzamide	EC50	0.5 nM	US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS
N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-(3-methyl-[1,2,4]triazolo[4,3-a]pyridin-8-yl)-2-oxopyrrolidin-3-yl]-4-(trifluoromethoxy)benzamide	EC50	0.5 nM	US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS
1-[(3R)-1-[3-chloro-4-(2-dimethylphosphorylphenyl)-2-fluorophenyl]-2-oxopyrrolidin-3-yl]-3-(4-chloro-2-fluorophenyl)urea	EC50	0.52 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.53 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-[(3R)-1-[4-(2-diethylphosphorylphenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]urea	EC50	0.53 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[2-cyclopropyl-4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopyrrolidin-3-yl]urea	EC50	0.55 nM	US-10676431: Phenylpyrrolidinone formyl peptide 2 receptor agonists

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 1225 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	affects expression, increases abundance, decreases expression	3
Nickel	decreases expression, increases expression	3
Calcitriol	affects cotreatment, decreases expression, increases expression	2
Dexamethasone	decreases reaction, increases expression, affects binding	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	decreases methylation, affects 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)

Via MONDO — disease-level, not drug-specific.

showing 60 of 485 trials:

NCT	Phase	Status	Title
NCT00152750	Phase 4	UNKNOWN	Study of Clonidine on Sleep Architecture in Children With Tourette’s Syndrome (TS) and Comorbid ADHD
NCT00226824	Phase 4	TERMINATED	Safety Study of Galantamine in Tic Disorders
NCT00241176	Phase 4	COMPLETED	Open Label Trial of Aripiprazole in Children and Adolescents With Tourette’s Disorder
NCT00370838	Phase 4	COMPLETED	Comparison of Keppra and Clonidine in the Treatment of Tics
NCT01018056	Phase 4	COMPLETED	Developing New Treatments for Tourette Syndrome: Therapeutic Trials With Modulators of Glutamatergic Neurotransmission
NCT01547000	Phase 4	COMPLETED	Guanfacine in Children With Tic Disorders
NCT03239210	Phase 4	COMPLETED	Effects of Ondansetron in Obsessive-compulsive and Tic Disorders
NCT00029224	Phase 4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	Phase 4	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	Phase 4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	Phase 4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	Phase 4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	Phase 4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	Phase 4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	Phase 4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	Phase 4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	Phase 4	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	Phase 4	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	Phase 4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	Phase 4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	Phase 4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	Phase 4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	Phase 4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	Phase 4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	Phase 4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	Phase 4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	Phase 4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	Phase 4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	Phase 4	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	Phase 4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	Phase 4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	Phase 4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	Phase 4	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	Phase 4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	Phase 4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	Phase 4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	Phase 4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	Phase 4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	Phase 4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	Phase 4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	Phase 4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	Phase 4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	Phase 4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	Phase 4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	Phase 4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	Phase 4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	Phase 4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer
NCT01673984	Phase 4	TERMINATED	GP Extended Action Triptorelin
NCT01753297	Phase 4	COMPLETED	A Study of Immediate 9 Months Adjuvant Hormone Therapy With Triptorelin 11.25 mg Versus Active Surveillance After Radical Prostatectomy in High Risk Prostate Cancer Patients.
NCT01794793	Phase 4	COMPLETED	Study to Allow Access to Pasireotide for Patients Benefiting From Pasireotide Treatment in Novartis-sponsored Studies
NCT01950871	Phase 4	TERMINATED	Prostate Guided Biopsy Study Evaluating the Diagnostic Performance of Prostate HistoScanning
NCT01995513	Phase 4	COMPLETED	Safety Study of Continued Enzalutamide Treatment In Prostate Cancer Patients
NCT02102646	Phase 4	COMPLETED	MRI Substudy; Metabolic Changes Due to Iatrogenic Hypogonadism
NCT02116582	Phase 4	COMPLETED	A Study to Evaluate Enzalutamide After Abiraterone in Metastatic Castration-Resistant Prostate Cancer
NCT02149628	Phase 4	COMPLETED	The Effect of Propofol Based Total Intravenous Anesthesia on Oxidative Stress and Nitric Oxide
NCT02405858	Phase 4	COMPLETED	A Study of Abiraterone Acetate in Metastatic Castration-Resistant Prostate Cancer Participants Who Responded Poorly to the First-line Combined Androgen Blockade Therapy
NCT02441517	Phase 4	TERMINATED	A Study of Enzalutamide Re-treatment in Metastatic Castration-resistant Prostate Cancer After Docetaxel and/or Cabazitaxel Treatment
NCT02441894	Phase 4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT02475057	Phase 4	COMPLETED	Endothelial Function in Prostate Cancer Patients on Degarelix vs. Luteinizing Hormone-Releasing Hormone Agonists
NCT02511665	Phase 4	UNKNOWN	Metformin And Longevity

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for FPR1 across ~30M SureChEMBL compounds — explore on Sugi Predict.