FPR2

Summary

FPR2 (formyl peptide receptor 2, HGNC:3827) is a protein-coding gene on chromosome 19q13.41, encoding N-formyl peptide receptor 2 (P25090). Pattern recognition G protein-coupled receptor (GPCR) that recognizes peptides with N-terminal formyl methionine, which are derived from invading pathogens or host mitochondria as pathogen or damage-associated molecular patterns (PAMPs and DAMPs).

Enables amyloid-beta binding activity; scavenger receptor binding activity; and signaling receptor activity. Involved in several processes, including cellular response to amyloid-beta; positive regulation of ERK1 and ERK2 cascade; and regulation of defense response. Located in cytoplasm and plasma membrane.

Source: NCBI Gene 2358 — automated summary from GO annotations (Alliance of Genome Resources).

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 48 total
• GTEx eGene: eQTL in 9 tissues, sQTL in 1 (q < 0.05)
• ChEMBL bioactivity: 4 clinical-phase molecules tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.08 (LoF-tolerant), LOEUF 1.67 (unconstrained)
• MANE Select transcript: NM_001005738

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3827
Approved symbol	FPR2
Name	formyl peptide receptor 2
Location	19q13.41
Locus type	gene with protein product
Status	Approved
Aliases	LXA4R, HM63, FPRH2, FMLPX, FPR2A, FMLP-R-II, ALXR, ALX
Ensembl gene	ENSG00000171049
Ensembl biotype	protein_coding
OMIM	136538
Entrez	2358

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 7 protein_coding

MANE Select: ENST00000340023

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 1, TSL 5: 3

ENST00000340023, ENST00000598776, ENST00000598953, ENST00000599326, ENST00000600258, ENST00000600722, ENST00001137417

RefSeq mRNA: 2 — MANE Select: NM_001005738 NM_001005738, NM_001462

CCDS: CCDS12840

Canonical transcript exons

ENST00000340023 — 2 exons

Exon	Start	End
ENSE00003127886	51761180	51761230
ENSE00003447537	51768645	51770531

Expression profiles

Bgee: expression breadth ubiquitous, 159 present calls, max score 95.55.

FANTOM5 (CAGE): breadth broad, TPM avg 8.0372 / max 1741.5119, expressed in 282 samples.

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

Genetic regulation across tissues (GTEx eQTL / sQTL)

FPR2 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 9 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

10 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Cells Cultured fibroblasts	eqtl	2.2e-33	+0.79	19:51743244:G:GCAGCTGGTGT
Whole Blood	sqtl	2.3e-22	-0.37	19:51762523:T:G
Whole Blood	eqtl	1.7e-03	-0.09	19:51750853:G:A
Testis	eqtl	9.5e-03	-0.17	19:51783432:G:A
Brain Nucleus accumbens basal ganglia	eqtl	1.0e-02	-0.29	19:51731454:G:A
Brain Anterior cingulate cortex BA24	eqtl	1.8e-02	+0.29	19:51717878:C:T
Skin Not Sun Exposed Suprapubic	eqtl	2.1e-02	-0.43	19:51045601:C:T
Esophagus Mucosa	eqtl	2.6e-02	+0.16	19:51743928:A:C
Muscle Skeletal	eqtl	3.1e-02	-0.18	19:51848753:C:T
Esophagus Gastroesophageal Junction	eqtl	4.1e-02	-0.25	19:51086216:T:C

FANTOM5 promoters

showing 10 of 11 alternative TSS:

Promoter ID	TPM avg	Samples expressed
177254	6.0474	225
177246	0.4681	51
177251	0.3439	92
177248	0.2738	38
177255	0.2388	56
177250	0.2301	88
177253	0.1836	60
208914	0.0713	28
177252	0.0639	43
177256	0.0583	13

Top tissues by expression

showing 100 of 284 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
blood	UBERON:0000178	95.55	gold quality
monocyte	CL:0000576	95.13	gold quality
leukocyte	CL:0000738	94.56	gold quality
mononuclear cell	CL:0000842	94.55	gold quality
granulocyte	CL:0000094	89.88	gold quality
bone marrow	UBERON:0002371	87.57	gold quality
Brodmann (1909) area 10	UBERON:0013541	86.00	silver quality
bone marrow cell	CL:0002092	85.63	gold quality
right lung	UBERON:0002167	83.22	gold quality
spleen	UBERON:0002106	83.00	gold quality
vermiform appendix	UBERON:0001154	80.83	gold quality
periodontal ligament	UBERON:0008266	78.93	gold quality
upper lobe of left lung	UBERON:0008952	78.92	gold quality
frontal pole	UBERON:0002795	77.76	gold quality
paraflocculus	UBERON:0005351	77.45	gold quality
upper lobe of lung	UBERON:0008948	77.26	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.22	gold quality
middle frontal gyrus	UBERON:0002702	76.91	silver quality
caecum	UBERON:0001153	74.14	gold quality
lung	UBERON:0002048	71.40	gold quality
gall bladder	UBERON:0002110	71.33	gold quality
endometrium epithelium	UBERON:0004811	70.59	gold quality
trabecular bone tissue	UBERON:0002483	68.04	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	66.89	gold quality
smooth muscle tissue	UBERON:0001135	66.61	gold quality
palpebral conjunctiva	UBERON:0001812	65.63	gold quality
left uterine tube	UBERON:0001303	65.62	gold quality
omental fat pad	UBERON:0010414	64.71	gold quality
peritoneum	UBERON:0002358	64.65	gold quality
adipose tissue of abdominal region	UBERON:0007808	63.99	gold quality
pancreatic ductal cell	CL:0002079	63.78	silver quality
lymph node	UBERON:0000029	62.30	gold quality
hindlimb stylopod muscle	UBERON:0004252	61.76	gold quality
lower lobe of lung	UBERON:0008949	60.51	silver quality
descending thoracic aorta	UBERON:0002345	60.39	gold quality
nasal cavity epithelium	UBERON:0005384	60.18	silver quality
endothelial cell	CL:0000115	59.59	gold quality
sperm	CL:0000019	59.37	gold quality
buccal mucosa cell	CL:0002336	59.29	gold quality
left adrenal gland cortex	UBERON:0035825	59.23	gold quality
right coronary artery	UBERON:0001625	58.91	gold quality
male germ cell	CL:0000015	58.82	gold quality
urinary bladder	UBERON:0001255	58.49	gold quality
left adrenal gland	UBERON:0001234	58.48	gold quality
mucosa of urinary bladder	UBERON:0001259	58.25	silver quality
right atrium auricular region	UBERON:0006631	57.55	gold quality
right ovary	UBERON:0002118	57.46	gold quality
adrenal cortex	UBERON:0001235	57.43	gold quality
liver	UBERON:0002107	57.42	gold quality
decidua	UBERON:0002450	57.35	gold quality
thoracic aorta	UBERON:0001515	57.33	gold quality
right adrenal gland	UBERON:0001233	57.24	gold quality
left coronary artery	UBERON:0001626	57.03	gold quality
cardiac atrium	UBERON:0002081	56.89	gold quality
right adrenal gland cortex	UBERON:0035827	56.81	gold quality
ascending aorta	UBERON:0001496	56.80	gold quality
coronary artery	UBERON:0001621	56.25	gold quality
heart left ventricle	UBERON:0002084	56.21	gold quality
adrenal gland	UBERON:0002369	56.06	gold quality
heart	UBERON:0000948	55.76	gold quality
subcutaneous adipose tissue	UBERON:0002190	55.73	gold quality
cardiac ventricle	UBERON:0002082	55.68	gold quality
right lobe of liver	UBERON:0001114	55.55	gold quality
adipose tissue	UBERON:0001013	55.52	gold quality
connective tissue	UBERON:0002384	55.27	gold quality
upper leg skin	UBERON:0004262	55.17	silver quality
placenta	UBERON:0001987	55.04	gold quality
mucosa of stomach	UBERON:0001199	54.88	gold quality
biceps brachii	UBERON:0001507	54.73	gold quality
myocardium	UBERON:0002349	54.42	gold quality
amniotic fluid	UBERON:0000173	54.36	gold quality
nasal cavity mucosa	UBERON:0001826	54.33	gold quality
hair follicle	UBERON:0002073	53.68	gold quality
thymus	UBERON:0002370	53.59	gold quality
oocyte	CL:0000023	53.54	gold quality
layer of synovial tissue	UBERON:0007616	53.18	silver quality
rectum	UBERON:0001052	52.54	gold quality
vastus lateralis	UBERON:0001379	52.51	gold quality
anatomical system	UBERON:0000467	52.37	gold quality
material anatomical entity	UBERON:0000465	52.26	gold quality
multicellular organism	UBERON:0000468	52.26	gold quality
ovary	UBERON:0000992	52.22	gold quality
left ovary	UBERON:0002119	51.96	gold quality
epithelial cell of pancreas	CL:0000083	51.85	gold quality
deltoid	UBERON:0001476	51.83	gold quality
medial globus pallidus	UBERON:0002477	51.78	gold quality
aorta	UBERON:0000947	51.77	gold quality
tibialis anterior	UBERON:0001385	51.17	silver quality
fallopian tube	UBERON:0003889	51.09	gold quality
muscle tissue	UBERON:0002385	50.88	gold quality
metanephric glomerulus	UBERON:0004736	50.71	gold quality
body of stomach	UBERON:0001161	50.54	gold quality
globus pallidus	UBERON:0001875	50.38	gold quality
myometrium	UBERON:0001296	50.37	gold quality
ileal mucosa	UBERON:0000331	50.18	silver quality
small intestine	UBERON:0002108	50.08	gold quality
renal glomerulus	UBERON:0000074	49.96	gold quality
left testis	UBERON:0004533	49.96	gold quality
small intestine Peyer’s patch	UBERON:0003454	49.91	gold quality
adult mammalian kidney	UBERON:0000082	49.86	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-MTAB-9801	yes	6.08
E-ANND-3	yes	4.00

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 63 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Appendix	tissue	52.9	medium
Bone marrow	tissue	15.6	medium
Spleen	tissue	14.8	low
Urinary bladder	tissue	14.0	not detected
Adipose tissue	tissue	12.7	not detected
Placenta	tissue	7.1	medium
Lung	tissue	6.8	not detected
Smooth muscle	tissue	6.2	not detected
Gallbladder	tissue	5.6	not detected
Liver	tissue	4.6	low
Tongue	tissue	3.9
Choroid plexus	tissue	2.7
Testis	tissue	2.2	not detected
Pancreas	tissue	2.1	low
Medulla oblongata	tissue	2.1
Lymph node	tissue	1.7	not detected
Esophagus	tissue	1.6	not detected
Putamen	tissue	1.6
Retrosplenial cortex	tissue	1.6
Thymus	tissue	1.5
Spinal cord	tissue	1.4
Nucleus accumbens	tissue	1.3
Small intestine	tissue	1.2	medium
Locus coeruleus	tissue	1.2
Hippocampus	tissue	1.2	not detected
Adrenal gland	tissue	1.1	medium
Substantia nigra	tissue	1.0
Duodenum	tissue	0.9	high
Colon	tissue	0.8	high
Tonsil	tissue	0.8	not detected
Fallopian tube	tissue	0.8	not detected
Ovary	tissue	0.7	not detected
Postcentral gyrus	tissue	0.7
Thyroid gland	tissue	0.6	low
Breast	tissue	0.5	not detected
Stomach 1	tissue	0.5	not detected
Endometrium 1	tissue	0.5	not detected
Cervix	tissue	0.4	not detected
Heart muscle	tissue	0.4	not detected
Salivary gland	tissue	0.4	not detected
Rectum	tissue	0.4	high
Kidney	tissue	0.4	not detected
Prostate	tissue	0.4	not detected
Skin 1	tissue	0.3	low
Vagina	tissue	0.3	not detected
Parathyroid gland	tissue	0.3	not detected
Basal ganglia	tissue	0.3	low
Midbrain	tissue	0.3
Ventral forebrain	tissue	0.3
Pituitary gland	tissue	0.2
Pons	tissue	0.2
Seminal vesicle	tissue	0.2	not detected
Skeletal muscle	tissue	0.2	not detected
Amygdala	tissue	0.2
Caudate putamen	tissue	0.2
Retina	tissue	0.1
Epididymis	tissue	0.1	not detected
Thalamus	tissue	0.1
Hypothalamus	tissue	0.1
Entorhinal cortex	tissue	0.1

Brain sub-regions (HPA Brain Atlas): detected in 184; highest nTPM — Area parastriata, superior (6.3), Anterior thalamic nucleus, ventral (3.3), Ventrolateral tegmental area, A5 NE cell group (2.7), Frontal operculum (2.6), Piriform cortex (2.6).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BHLHA15, CREBZF, TAL1

miRNA regulators (miRDB)

Targeting FPR2 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 47 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-6755-5P	99.95	65.59	464
HSA-MIR-144-3P	99.94	73.98	2698
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-9902	99.89	69.15	2250
HSA-MIR-548AZ-5P	99.83	69.94	3230
HSA-MIR-548T-5P	99.83	69.91	3220
HSA-MIR-3121-3P	99.82	71.96	3630
HSA-MIR-548AV-5P	99.60	70.84	2107
HSA-MIR-548K	99.60	70.84	2107
HSA-MIR-885-5P	99.59	68.59	879
HSA-MIR-451B	99.55	68.28	1380
HSA-MIR-3120-3P	99.54	70.28	2669
HSA-MIR-3609	99.52	69.89	2587
HSA-MIR-548AH-5P	99.52	69.73	2626
HSA-MIR-543	99.52	69.03	2595
HSA-MIR-7159-3P	99.51	70.17	1920
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-8054	99.48	70.81	2084
HSA-MIR-4666A-5P	99.41	69.72	1887
HSA-MIR-3140-5P	99.39	69.04	1136
HSA-MIR-4427	99.34	70.33	1854
HSA-MIR-580-5P	99.28	70.94	1776
HSA-MIR-1264	99.25	66.81	1317
HSA-MIR-122B-3P	99.21	68.90	1333

Functional genomics

gnomAD constraint: pLI 0.0787, LOEUF 1.67, missense Z 1.45 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000340023 — one region, missense o/e 0.85.

Literature-anchored findings (GeneRIF, showing 40)

• chemoattractant Trp-Lys-Tyr-Met-Val-D-Met activates eosinophils through the formyl peptide receptor and one of its homologues, formyl peptide receptor-like 1 (PMID:12377951)
• results indicate that the cytokine-like property of serum amyloid A is manifested through activation of the Gi-coupled formyl peptide receptor-like 1(FPRL1/LXA4R) (PMID:12393391)
• 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)
• LXA(4) generated in or near the paracellular space via neutrophil-epithelial interactions can rapidly act on epithelial LXA(4)receptor to downregulate epithelial promotion of intestinal inflammation. (PMID:12456400)
• Modulation of neutrophil FPRL1 by distinct peptide ligands activates a spectrum of cellular signaling events, including intracellular calcium concentration increase, phosphoinositide 3-kinase, extracellular signal-regulated kinase, and Akt activation. (PMID:14662886)
• 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)
• The up-regulation of the A-SAA and FPRL1 genes in inflamed synovial tissue suggests an important role in the pathophysiology of inflammatory arthritis (PMID:15188355)
• ligand-bound FPRL1 undergoes primarily clathrin-mediated and dynamin-dependent endocytosis (PMID:15224191)
• Results show that humanin (HN) acts as a ligand for formyl peptide receptor-like 1 (FPRL1) and 2 (FPRL2). (PMID:15465011)
• FPR and FPRL1, use distinct signaling pathways in activation of human neutrophils (PMID:15625007)
• results showed that multiple domains in FPRL1 are involved in the receptor response to chemotactic agonists with the sixth transmembrane domain and the third extracellular loop playing a prominent role (PMID:15670157)
• serum amyloid A plays a role in the modulation of inflammatory and immune responses via FPRL1, by inducing matrix-metalloproteinase-9 upregulation (PMID:15809093)
• cells transfected with FPRL1 gene exhibited markedly reduced tumorigenicity in syngeneic mice (PMID:15829413)
• FPRL1 is a pituitary adenylate cyclase activating polypeptide (PACAP) 27-specific receptor. (PMID:16493055)
• In view of the wide range of endogenous ligands known to interact with FPRL-1, including the anti-inflammatory protein annexin-A1, we speculate that the novel effect here described may impact on the clinical immunosuppressive (PMID:16973129)
• binding of SAA to FPRL1 may contribute to the destruction of bone and cartilage via the promotion of synoviocyte hyperplasia and angiogenesis (PMID:17015746)
• Analysis of in vitro expression of lipoxin A(4) receptor (ALX) on human neutrophils and the in vivo anti-inflammatory effect of glucocorticoids. (PMID:17184966)
• 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)
• association of the PDGFRbeta with lipid raft microdomains renders it susceptible to LXA(4)-mediated dephosphorylation by possible reactivation of oxidatively inactivated SHP-2. (PMID:17403678)
• Exocytosis of FPRL1 results in down-regulation of cytoplasmic FRPL1 in patients with pyoderma. (PMID:17460114)
• Both intra- and extracellular Ca2+ play a role in controlling pro-inflammatory functions stimulated by PACAP which acts through a VPAC-1, FPRL1/Galphai/PI3K/ERK pathway and a VPAC-1/Galphas/PKA/p38 pathway to fully activate monocytes (PMID:17651798)
• To specifically inhibit the FPRL1 response the antagonist WRW(4) should be used. (PMID:17687636)
• 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)
• FPRL-1 is capable of activating nuclear factor-kappa B (NF-kappaB) signaling through inhibitor-kappa B kinase (IKK) phosphorylation in human astrocytoma or Chinese hamster ovary cells. (PMID:17727628)
• level of LXA4 in synovial fluid and lipoxin A4 receptor expression in synovial tissues obtained from patients with rheumatoid arthritis and osteoarthritis (PMID:17918787)
• Proinflammatory effect of VIP is mediated via the specific G protein-coupled receptor VIP/pituitary adenylate cyclase-activating protein (VPAC1) receptor as well as via FPRL1. (PMID:18174366)
• Our results indicate that severe asthma is characterized by decreased airway LXA4 levels and luekocyte AKX receptor availability. (PMID:18583575)
• FPRL1 is a potent mediator in the activation of CRAC channels (PMID:18652801)
• The chemokine FPRL1 plays a role in the production of chemokine CCL2 by serum amyloid A. (PMID:18768891)
• Data show that MMK-1 is a member of a group of FPR2 ligands that activate the neutrophil superoxide-generating NADPH-oxidase. (PMID:19282028)
• FPRL1-induced chemotactic migration and IL-1 beta production from human phagocytes was ihibited by lysophosphatidylglycerol. (PMID:19381066)
• These results suggest that CCR3 may be used as a surrogate co-receptor by subtype B while FPRL1 may be used as a surrogate co-receptor by subtypes A and C HIV-1. (PMID:19553323)
• LXA(4) does not act through FPR2 in neutrophils. (PMID:19751275)
• ECRG2 regulates invasion/migration partly through ECM degradation and uPA/uPAR/FPRL1 pathway (PMID:19796867)
• both LxA4 and a chemotactic lipid leishmania chemotactic factor released by the parasite leishmania increased infectivity of this pathogen in an lipoxin A4 receptor dependent fashion (PMID:19811292)
• All tested samples of human natural killer (NK) cells express FPR2; activation of FPR2 elicits cytolytic activity and chemotactic migration of NK cells. (PMID:19843937)
• The results indicate that SAA stimulates FPR2-mediated activation of p38 MAPK and JNK, which are independent of a pertussis toxin-sensitive G-protein and are essential for SAA-induced CCL2 production. (PMID:20177146)
• These data demonstrate that the human formyl peptide receptor 2 (FPR2/ALX) senses phenol-soluble modulins at nanomolar concentrations and initiates proinflammatory neutrophil responses to community acquired MRSA. (PMID:20542250)
• promoter polymorphism is associated with chronic urticaria in a Korean population (PMID:20642210)
• 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)

Cross-species orthologs

11 orthologs

Organism	Symbol	Gene ID
mus_musculus	Fpr-rs4	ENSMUSG00000048062
mus_musculus	Fpr2	ENSMUSG00000052270
mus_musculus	Fpr-rs3	ENSMUSG00000060701
mus_musculus	Fpr-rs6	ENSMUSG00000071275
mus_musculus	Fpr-rs7	ENSMUSG00000071276
mus_musculus	Fpr3	ENSMUSG00000079700
rattus_norvegicus	Fpr3	ENSRNOG00000031331
rattus_norvegicus	Fpr2	ENSRNOG00000042605
rattus_norvegicus	Fpr2l2	ENSRNOG00000043056
rattus_norvegicus	Fpr2l1	ENSRNOG00000045732
rattus_norvegicus	Fpr2l2	ENSRNOG00000079547

Paralogs (8): C5AR2 (ENSG00000134830), GPR32 (ENSG00000142511), FPR1 (ENSG00000171051), C3AR1 (ENSG00000171860), CMKLR1 (ENSG00000174600), FPR3 (ENSG00000187474), C5AR1 (ENSG00000197405), GPR33 (ENSG00000214943)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1278319) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 35 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal dendritic cell physiology	2
impaired macrophage chemotaxis	2
decreased dendritic cell number	2
abnormal colon morphology	1
intestinal ulcer	1
decreased inflammatory response	1
increased colon adenoma incidence	1
small lymph nodes	1
respiratory system inflammation	1
abnormal innate immunity	1
decreased immunoglobulin level	1
abnormal neutrophil physiology	1
decreased IgE level	1
colitis	1
abnormal cytokine secretion	1
increased susceptibility to induced arthritis	1
increased incidence of tumors by chemical induction	1
abnormal large intestine crypts of Lieberkuhn morphology	1
decreased acute inflammation	1
increased acute inflammation	1
abnormal response to injury	1
decreased IgG1 level	1
decreased IgG2b level	1
decreased susceptibility to induced colitis	1
decreased interferon-gamma secretion	1

+10 more (showing top 25).

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 troglodytes	P60019	100.0%	Diamond
Pan paniscus	Q3SAG9	100.0%	Diamond
Gorilla gorilla gorilla	Q6XCF2	100.0%	Diamond
Macaca mulatta	O97664	99.2%	Diamond
Macaca fascicularis	Q95LH1	99.2%	Diamond
Pongo pygmaeus	P79234	97.9%	Diamond
Meleagris gallopavo	O93361	97.6%	Diamond
Gallus gallus	Q98907	97.6%	Diamond
Pongo abelii	Q5REI5	96.5%	Diamond
Meriones unguiculatus	Q99PE4	93.6%	Diamond
Hoolock hoolock	Q4QXU6	92.4%	Diamond
Rattus rattus	Q49SP8	89.4%	Diamond
Sus scrofa	B1PHQ8	87.4%	Diamond
Bos taurus	B9VR26	85.4%	Diamond
Oryctolagus cuniculus	Q05394	79.2%	Diamond
Canis lupus familiaris	P30992	69.8%	Diamond
Cavia porcellus	O70129	68.9%	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
FPR1	protein-coding	2357
FPR3	protein-coding	2359
ZNF577	protein-coding	84765
SPACA6-AS1	ncRNA	102238594
SPACA6	protein-coding	147650
HAS1	protein-coding	3036
MIR125A	ncRNA	406910
ZNF649-AS1	ncRNA	101928571
ZNF649	protein-coding	65251

Protein

Protein identifiers

N-formyl peptide receptor 2 — P25090 (reviewed: P25090)

Alternative names: FMLP-related receptor I, Formyl peptide receptor-like 1, HM63, Lipoxin A4 receptor, RFP

All UniProt accessions (4): P25090, M0QXD3, M0QZ89, M0R222

UniProt curated annotations — full annotation on UniProt →

Function. Pattern recognition G protein-coupled receptor (GPCR) that recognizes peptides with N-terminal formyl methionine, which are derived from invading pathogens or host mitochondria as pathogen or damage-associated molecular patterns (PAMPs and DAMPs). Preferentially recognizes longer peptides or peptides with specific sequences such as the phenol-soluble modulin (PSM) family of formylated peptide toxins produced by Staphylococcus aureus. Ligand binding causes a conformation change that triggers signaling via G(i)/GNAI1 inhibiting adenylate cyclase activity, leading to decreased intracellular cAMP levels. In addition, can recognize a variety of chemically distinct endogenous ligands including proteins and lipids besides formylpeptides and thereby plays multiple roles in inflammation. Acts as a receptor for the chemokine-like protein FAM19A5, mediating FAM19A5-stimulated macrophage chemotaxis and the inhibitory effect on TNFSF11/RANKL-induced osteoclast differentiation. Acts also as a ceramide membrane receptor, and long-chain ceramides (C14 to C20) binding induces conformational changes that inhibits diet-induced adipose thermogenesis. Participates in neuroprotection via interaction with humanin/MT-RNR2 and Amyloid-beta protein 42, product of APP. Differential signaling is also defined by receptor oligomerization state. Binding of ANXA1 to FPR2 homodimer elicits activation of p38 MAPKinase pathway leading to HSPB1/HSP27 phosphorylation and IL10 production in monocytes. Whereas agonistic activation of FPR1:FPR2 heterodimers signals a proapoptotic JNK pathway in neutrophils.

Subunit / interactions. Homodimer; the homodimerization is potentiated in response to the anti-inflammatory agonist ANXA1 and inhibited upon binding of pro-inflammatory agonist serum amyloid A. Heterodimer with FPR1; the heterodimerization with FPR1 is potentiated in response to anti-inflammatory agonists such as lipoxin A4, ANXA1 and Ac2-26 ANXA1 peptide. Forms a complex with heterotrimeric G(i) protein composed of GNAI1, GNB1 and GNG2 subunits. Interacts with amyloid-beta protein 42, product of APP; the interaction takes place at the cell surface and the complex is then rapidly internalized. Interacts with S1PR4. Interacts with GNAI1. Interacts with humanin/MT-RNR2. Interacts with GNAI2. (Microbial infection) Interacts with Staphylococcus aureus protein SSL13; this interaction leads to the activation of neutrophils.

Subcellular location. Cell membrane.

Tissue specificity. Detected in lung, bone marrow, neutrophils, spleen and testis.

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

RefSeq proteins (2): NP_001005738, NP_001453 (=MANE)

Domains & families (InterPro)

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

Pfam: PF00001

UniProt features (54 total): helix 21, topological domain 8, strand 8, transmembrane region 7, binding site 3, chain 1, region of interest 1, compositionally biased region 1, glycosylation site 1, disulfide bond 1, sequence conflict 1, turn 1

Structure

Experimental structures (PDB)

13 structures by resolution:

PDB	Title	Method	Resolution (Å)
8ZBW	Cryo-EM structure of formyl peptide receptor 2/C1R receptor in complex with Gi	ELECTRON MICROSCOPY	2.58
6LW5	Crystal structure of the human formyl peptide receptor 2 in complex with WKYMVm	X-RAY DIFFRACTION	2.8
7WVX	Cryo-EM structure of the human formyl peptide receptor 2 in complex with fhumanin and Gi2	ELECTRON MICROSCOPY	2.8
7T6U	Structure of the human FPR2-Gi complex with CGEN-855A	ELECTRON MICROSCOPY	2.9
7WVV	Cryo-EM structure of the human formyl peptide receptor 2 in complex with fMLFII and Gi2	ELECTRON MICROSCOPY	2.9
7T6S	Structure of the human FPR2-Gi complex with compound C43	ELECTRON MICROSCOPY	3
7WVY	Cryo-EM structure of the human formyl peptide receptor 2 in complex with Abeta42 and Gi2	ELECTRON MICROSCOPY	3
7T6V	Structure of the human FPR2-Gi complex with fMLFII	ELECTRON MICROSCOPY	3.1
7WVW	Cryo-EM structure of the human formyl peptide receptor 2 in complex with fMYFINILTL and …	ELECTRON MICROSCOPY	3.1
6OMM	Cryo-EM structure of formyl peptide receptor 2/lipoxin A4 receptor in complex with Gi	ELECTRON MICROSCOPY	3.17
8Y62	Cryo-EM structure of the C16:0 ceramide-bound FPR2-Gi complex	ELECTRON MICROSCOPY	3.2
8Y63	Cryo-EM structure of the C20:0 ceramide-bound FPR2-Gi complex	ELECTRON MICROSCOPY	3.2
9JHJ	Cryo-EM structure of the C18:0 ceramide-bound FPR2-Gi complex	ELECTRON MICROSCOPY	3.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P25090-F1	84.87	0.66

Antibody-complex structures (SAbDab)

6 antibodies co-crystallized with this protein: 6OMM, 7T6S, 7T6U, 7T6V, 8Y62, 9JHJ

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

Antibody reliability (HPA): IH 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 (3)

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

Disulfide bonds (1)

Type	Positions
Disulfide bond	98–176

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	4

Function

Pathways and Gene Ontology

Reactome pathways

4 curated (TAS) of 12; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

12 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-416476	G alpha (q) signalling events	curated
R-HSA-6798695	Neutrophil degranulation	curated
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
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	—

MSigDB gene sets: 346 (showing top): GSE45365_NK_CELL_VS_CD11B_DC_DN, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_POSITIVE_REGULATION_OF_ENDOCYTOSIS, GOBP_MYELOID_LEUKOCYTE_MIGRATION, MORF_MSH3, GOBP_CELL_CHEMOTAXIS, MODULE_255, GOBP_INFLAMMATORY_RESPONSE, GOCC_SECRETORY_GRANULE, MODULE_45, MODULE_64, MORF_BRCA1, GOBP_REGULATION_OF_SUPEROXIDE_ANION_GENERATION

GO Biological Process (30): microglial cell activation (GO:0001774), complement receptor mediated signaling pathway (GO:0002430), immune response-regulating cell surface receptor signaling pathway (GO:0002768), receptor-mediated endocytosis (GO:0006898), chemotaxis (GO:0006935), inflammatory response (GO:0006954), cell adhesion (GO:0007155), cell surface receptor signaling pathway (GO:0007166), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), calcium-mediated signaling (GO:0019722), positive regulation of superoxide anion generation (GO:0032930), defense response to bacterium (GO:0042742), innate immune response (GO:0045087), positive regulation of innate immune response (GO:0045089), astrocyte activation (GO:0048143), negative regulation of inflammatory response (GO:0050728), positive regulation of phagocytosis (GO:0050766), positive chemotaxis (GO:0050918), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), positive regulation of ERK1 and ERK2 cascade (GO:0070374), positive regulation of monocyte chemotaxis (GO:0090026), dentinogenesis (GO:0097187), cellular response to amyloid-beta (GO:1904646), immune system process (GO:0002376), cell communication (GO:0007154), signal transduction (GO:0007165), signaling (GO:0023052)

GO Molecular Function (9): amyloid-beta binding (GO:0001540), complement receptor activity (GO:0004875), G protein-coupled receptor activity (GO:0004930), N-formyl peptide receptor activity (GO:0004982), scavenger receptor binding (GO:0005124), signaling receptor activity (GO:0038023), cargo receptor activity (GO:0038024), RAGE receptor binding (GO:0050786), protein binding (GO:0005515)

GO Cellular Component (6): cytoplasm (GO:0005737), plasma membrane (GO:0005886), membrane (GO:0016020), specific granule membrane (GO:0035579), tertiary granule membrane (GO:0070821), ficolin-1-rich granule membrane (GO:0101003)

Reactome top-level categories

8 top-level categories:

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

GO top-level categories

59 GO namespaces:

Category	Terms
secretory granule membrane	3
glial cell activation	2
vesicle-mediated transport	2
defense response	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
transmembrane signaling receptor activity	2
signaling receptor binding	2
cellular anatomical structure	2
tertiary granule	2
leukocyte activation involved in inflammatory response	1
macrophage activation	1
immune response-activating cell surface receptor signaling pathway	1
immune response-regulating signaling pathway	1
cell surface receptor signaling pathway	1
endocytosis	1
response to chemical	1
taxis	1
cellular process	1
G protein-coupled receptor activity	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
phospholipase C activator activity	1
regulation of biological quality	1
intracellular signaling cassette	1
regulation of superoxide anion generation	1
superoxide anion generation	1
positive regulation of reactive oxygen species metabolic process	1
response to bacterium	1
immune response	1
defense response to symbiont	1
positive regulation of response to biotic stimulus	1
positive regulation of defense response	1
positive regulation of response to external stimulus	1
innate immune response	1
regulation of innate immune response	1
positive regulation of immune response	1
astrocyte development	1
inflammatory response	1
negative regulation of defense response	1
negative regulation of response to external stimulus	1
regulation of inflammatory response	1
phagocytosis	1
positive regulation of endocytosis	1
regulation of phagocytosis	1
peptide binding	1
complement binding	1
complement receptor mediated signaling pathway	1
immune receptor activity	1
G protein-coupled peptide receptor activity	1
molecular transducer activity	1
molecular_function	1
molecular adaptor activity	1
binding	1
intracellular anatomical structure	1
membrane	1
cell periphery	1
specific granule	1
ficolin-1-rich granule	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 17 of 45 annotations. The rest are phylogenetic / computational / electronic (IEA).

17 experimentally-supported GO terms:

GO term	NS	Evidence
G protein-coupled receptor signaling pathway	BP	genetic interaction
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	BP	genetic interaction
calcium-mediated signaling	BP	genetic interaction
cell surface receptor signaling pathway	BP	direct assay
cellular response to amyloid-beta	BP	direct assay
defense response to bacterium	BP	direct assay
immune response-regulating cell surface receptor signaling pathway	BP	direct assay
negative regulation of inflammatory response	BP	direct assay
positive regulation of ERK1 and ERK2 cascade	BP	mutant phenotype
positive regulation of innate immune response	BP	direct assay
positive regulation of monocyte chemotaxis	BP	genetic interaction
positive regulation of phagocytosis	BP	direct assay
cytoplasm	CC	direct assay
plasma membrane	CC	direct assay
amyloid-beta binding	MF	physical interaction
scavenger receptor binding	MF	physical interaction
signaling receptor activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 1,592 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FPR2	ANXA1	P04083	931
FPR2	CAMP	P49913	849
FPR2	HSH2D	Q96JZ2	720
FPR2	TRIM11	Q96F44	663
FPR2	PLEKHF1	Q96S99	651
FPR2	PRNP	P04156	597
FPR2	DEFB4A	O15263	574
FPR2	APP	P05067	566
FPR2	SOCS2	O14508	551
FPR2	IL1B	P01584	549
FPR2	PRTN3	P15637	544
FPR2	TLR2	O60603	535
FPR2	GAPDH	P00354	528
FPR2	PYCR1	P32322	506
FPR2	ING1	Q9UK53	502

IntAct

Human interaction partners of FPR2 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

11 partners by confidence:

Partner	Interaction type	MIscore	Records
ARL6IP5	association	0.640	1
APOD	physical association	0.560	3
APP	physical association	0.560	3
FXYD6	physical association	0.560	3
LRRC25	physical association	0.560	3
SSMEM1	physical association	0.560	3
RAMP1	physical association	0.400	1
RAMP2	physical association	0.400	1
RAMP3	physical association	0.400	1
GPR89A	association	0.350	2
SCAMP3	association	0.350	1

BioGRID (197 interactions; top human partners by supporting records): ALG10 (Affinity Capture-MS; 2 records), ARAP1 (Affinity Capture-MS; 2 records), ARL6IP1 (Affinity Capture-MS; 2 records), ARL6IP5 (Affinity Capture-MS; 2 records), ATP12A (Affinity Capture-MS; 2 records), ATP2B2 (Affinity Capture-MS; 2 records), ATP2B3 (Affinity Capture-MS; 2 records), ATP2B4 (Affinity Capture-MS; 2 records), ATP5B (Affinity Capture-MS; 2 records), ATP8 (Affinity Capture-MS; 2 records), ATP9A (Affinity Capture-MS; 2 records), C4orf32 (Affinity Capture-MS; 2 records), CAMLG (Affinity Capture-MS; 2 records), CCDC132 (Affinity Capture-MS; 2 records), CERS5 (Affinity Capture-MS; 2 records)

SIGNOR signaling

5 signaling interactions:

A	Effect	B	Mechanism
FPR2	“up-regulates activity”	GNAI3	binding
FPR2	“up-regulates activity”	GNA14	binding
WKYMVm	“up-regulates activity”	FPR2	“chemical activation”
ANXA1	“up-regulates activity”	FPR2	binding
CAMP	up-regulates	FPR2	binding

Ligand–receptor pairs (CellPhoneDB) (8)

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

8 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
ALOX12	receptor	Signaling by Lipoxin/Leukotriene
ALOX5;ALOX5AP;LTC4S	receptor	Signaling by Lipoxin/Leukotriene
ANXA1	receptor	Signaling by Annexin
MT-RNR2	receptor	Signaling by Humanin
CCL23	receptor	Signaling by Chemokines
SAA1	receptor
TAFA5	receptor	Signaling by TAFA
APP	receptor	Signaling by Amyloid-beta precursor protein

Disease & clinical

Genetic variants

Variant evidence for FPR2: 48 ClinVar records (0 pathogenic / likely pathogenic); 4 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	42
Likely benign	3
Benign	2

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 18 predictions of 113):

Position(s)	Effect	Δscore	Sites
19:51761231–51761232	donor_loss	1.0000	2
19:51761231–51761232	donor_loss	0.9900	3
19:51763442	donor_gain	0.9900
19:51768643–51768644	acceptor_loss	0.9800	6
19:51768642	acceptor_loss	0.9600
19:51761212	donor_gain	0.8600
19:51767350	donor_gain	0.8100
19:51767354	donor_gain	0.8100
19:51768633	acceptor_gain	0.8000
19:51763490	donor_gain	0.7800

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Disease associations

OMIM: gene MIM:136538 | disease phenotypes:

Genomics England panels (PanelApp)

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

1 panels:

Panel	Rating
COVID-19 research	green

GWAS associations

4 associations:

Study	Trait	p-value
GCST007277_24	Tourette syndrome	9e-7
GCST009597_290	Multiple sclerosis	2e-6
GCST005531_87	Multiple sclerosis	3e-6
GCST004866_7	Alopecia areata	6e-6

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3038479 (PROTEIN FAMILY), CHEMBL4227 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 79,876 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

4 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1707	LOPERAMIDE HYDROCHLORIDE	4	59,642
CHEMBL422	TRIFLUOPERAZINE	4	20,190
CHEMBL6056273	IDREBORMILAST	2	19
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 (40 total), top 25:

Ligand	Action	Affinity	Parameter
LXA4	Full agonist	12.0	pEC50
resolvin D1	Full agonist	11.9	pEC50
RvD1-ME	Full agonist	11.43	pEC50
aspirin-triggered resolvin D1	Full agonist	11.1	pEC50
WKYMVm	Full agonist	10.13	pKd
MHC binding peptide	Full agonist	10.0	pIC50
BMS-986331	Agonist	9.3	pEC50
[3H]LXA4	Full agonist	9.3	pKd
sCKβ8-1	Full agonist	9.13	pEC50
MMK-1	Full agonist	8.7	pEC50
PSMα3	Full agonist	8.67	pEC50
ACT-389949	Agonist	8.52	pEC50
humanin	Full agonist	8.46	pEC50
BMS-986235	Agonist	8.3	pEC50
fMet-Met-Tyr-Ala-Leu-Phe	Full agonist	7.82	pEC50
SHAAGtide	Full agonist	7.72	pEC50
compound 43 [PMID: 21173551]	Full agonist	7.4	pEC50
T21/DP107	Full agonist	7.3	pEC50
compound 1754-31 [PMID: 23788657]	Antagonist	7.09	pIC50
uPar fragment	Full agonist	7.08	pEC50
PBP10	Antagonist	7.0	pIC50
amyloid β	Full agonist	7.0	pEC50
CRAMP	Full agonist	7.0	pEC50
CGEN-855A	Full agonist	6.72	pIC50
fMet-Ile-Val-Thr-Leu-Phe	Full agonist	6.7	pEC50

Binding affinities (BindingDB)

1657 measured of 2048 human assays (2080 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
CHEMBL5271637	EC50	0.02 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
CHEMBL4440913	IC50	0.1 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
CHEMBL5288361	EC50	0.13 nM
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
CHEMBL5281870	EC50	0.17 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
CHEMBL4794375	EC50	0.25 nM
CHEMBL5287715	EC50	0.25 nM
diethyl ({[(2S)-2-{[(4- bromophenyl)carbamoyl]amino} pentanoyl]amino}methyl) phosphonate	EC50	0.27 nM	US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
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
CHEMBL5273168	EC50	0.27 nM
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
CHEMBL5275581	EC50	0.29 nM
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

ChEMBL bioactivities

2892 potent at pChembl≥5 of 2991 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	EC50	0.01	nM	CHEMBL5556956
10.70	EC50	0.02	nM	CHEMBL5271637
10.30	EC50	0.05	nM	CHEMBL4776349
10.30	IC50	0.05	nM	CHEMBL5268572
10.15	EC50	0.07	nM	CHEMBL3730217
10.15	EC50	0.07	nM	CHEMBL552527
10.15	EC50	0.07	nM	CHEMBL5567819
10.11	EC50	0.078	nM	CHEMBL4790836
10.11	EC50	0.077	nM	CHEMBL5542293
10.07	EC50	0.085	nM	CHEMBL4743917
10.06	EC50	0.087	nM	CHEMBL4755590
10.05	EC50	0.09	nM	CHEMBL5558065
10.04	EC50	0.092	nM	CHEMBL4744094
10.00	EC50	0.1	nM	CHEMBL3728769
10.00	IC50	0.1	nM	CHEMBL4440913
10.00	EC50	0.1	nM	CHEMBL6168024
10.00	EC50	0.1	nM	CHEMBL6171866
9.96	EC50	0.11	nM	CHEMBL4784400
9.96	EC50	0.11	nM	CHEMBL4758920
9.92	IC50	0.12	nM	CHEMBL5268572
9.89	EC50	0.13	nM	CHEMBL3729012
9.89	EC50	0.13	nM	CHEMBL5288361
9.89	EC50	0.13	nM	CHEMBL5550062
9.85	EC50	0.14	nM	CHEMBL4781596
9.85	EC50	0.14	nM	CHEMBL5284349
9.85	EC50	0.14	nM	CHEMBL5612530
9.85	EC50	0.14	nM	CHEMBL6160913
9.82	EC50	0.15	nM	CHEMBL4744835
9.82	EC50	0.15	nM	CHEMBL5284349
9.80	EC50	0.16	nM	CHEMBL3727613
9.80	EC50	0.16	nM	CHEMBL4762030
9.77	EC50	0.17	nM	CHEMBL5281870
9.77	EC50	0.17	nM	CHEMBL6028833
9.77	EC50	0.17	nM	CHEMBL6001886
9.74	EC50	0.18	nM	CHEMBL4744094
9.74	EC50	0.18	nM	CHEMBL5564103
9.72	EC50	0.19	nM	CHEMBL4761554
9.72	EC50	0.19	nM	CHEMBL6173514
9.70	EC50	0.2	nM	CHEMBL3728932
9.70	EC50	0.2	nM	CHEMBL5614343
9.70	EC50	0.2	nM	CHEMBL5550062
9.68	EC50	0.21	nM	CHEMBL5270733
9.68	EC50	0.21	nM	CHEMBL6159963
9.66	EC50	0.22	nM	CHEMBL5923729
9.66	IC50	0.22	nM	CHEMBL5268572
9.64	EC50	0.23	nM	CHEMBL6172222
9.62	EC50	0.24	nM	CHEMBL3729214
9.62	IC50	0.24	nM	CHEMBL5289939
9.60	EC50	0.25	nM	CHEMBL4794375
9.60	EC50	0.25	nM	CHEMBL5287715

PubChem BioAssay actives

729 with measured affinity, of 1707 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-(4-chlorophenyl)-3-[(3S,4R)-1-(2-hydroxyethyl)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	<0.0001	uM
1-[(7R,8S)-7-(2,6-difluoro-4-methoxyphenyl)-4,6,7,8-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]oxadiazin-8-yl]-3-(4-fluorophenyl)urea	1932218: Agonist activity at FPR2 (unknown origin) assessed as increase in calcium flux	ec50	<0.0001	uM
1-(4-chloro-3-hydroxyphenyl)-3-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-(4-chlorophenyl)-3-[(3S,4R)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-(4-fluorophenyl)-3-[(3S,4R)-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3S,4R)-4-(2,5-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3S,4R)-1-ethyl-4-(4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1932219: Agonist activity at human FPR2 expressed in HEK293 cells assessed as increase in calcium flux incubated for 45 mins by Fluo-4 AM dye based fluorescence assay	ec50	0.0001	uM
1-(4-chlorophenyl)-3-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluoro-3-hydroxyphenyl)urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(3-hydroxy-4-methylphenyl)urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2127414: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin -induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0001	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0001	uM
1-(4-chlorophenyl)-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]urea	1932216: Agonist activity at human FPR2 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay	ec50	0.0001	uM
methyl (E,5S,6R)-5,6-dihydroxy-8-[5-[(1S)-1-hydroxyhexyl]-1,2-dimethylimidazol-4-yl]oct-7-enoate	1585249: Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-12p70 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay	ic50	0.0001	uM
1-(4-chlorophenyl)-3-[(3S,4S)-4-(4-methoxyphenyl)-2-oxopiperidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0001	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphoryl-3-fluorophenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0001	uM
1-[(3R)-1-[4-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]urea	2231656: Agonist activity at human FPR2 expressed in forskolin/IBMX-treated CHO cells incubated for 30 mins by HTRF HiRange cAMP assay	ec50	0.0001	uM
1-(4-chlorophenyl)-3-[(3S,4S)-3-(4-methoxyphenyl)-1-[(1-methylsulfonylpyrazol-4-yl)methyl]piperidin-4-yl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0001	uM
(2R,3R)-3-N-(4-bromophenyl)-2-N-(4-piperidin-1-ylbutyl)spiro[bicyclo[2.2.1]heptane-7,1’-cyclopropane]-2,3-dicarboxamide	2083663: Agonist activity at FPR2 (unknown origin) in HEK293 cells	ec50	0.0001	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R,5S)-1-[2,3-difluoro-4-[3-(trifluoromethyl)pyrrolidin-1-yl]phenyl]-5-(hydroxymethyl)-2-oxopyrrolidin-3-yl]urea	2231656: Agonist activity at human FPR2 expressed in forskolin/IBMX-treated CHO cells incubated for 30 mins by HTRF HiRange cAMP assay	ec50	0.0001	uM
N-[[1-[2,3-difluoro-4-[(3R)-3-[[2-fluoro-4-(trifluoromethyl)phenyl]carbamoylamino]-2-oxopyrrolidin-1-yl]phenyl]cyclopropyl]methyl]-N-methylacetamide	2270773: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin-induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0001	uM
(2S)-6-amino-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]hexanamide	2083635: Agonist activity at human FPR2	ec50	0.0001	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(3,4-difluorophenyl)urea	1720303: Agonist activity at human FPR2 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	0.0002	uM
1-[(3R)-1-[4-[1-(methanesulfonamidomethyl)cyclopropyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	1932216: Agonist activity at human FPR2 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay	ec50	0.0002	uM
1-[(3R)-1-[4-[3-(dimethylamino)piperidin-1-yl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0002	uM
1-(4-bromophenyl)-3-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0002	uM
1-(4-chlorophenyl)-3-[(1S)-1-[5-(2-hydroxyethyl)-1,2,4-oxadiazol-3-yl]-2-(4-methoxyphenyl)ethyl]urea	1932219: Agonist activity at human FPR2 expressed in HEK293 cells assessed as increase in calcium flux incubated for 45 mins by Fluo-4 AM dye based fluorescence assay	ec50	0.0002	uM
1-(4-chlorophenyl)-3-[(3R)-1-[4-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea	2264869: Agonist activity at human FPR2 receptor expressed in CHO cells assessed as forskolin/IBMX-induced intracellular cAMP level incubated for 30 mins by HTRF HiRange cAMP assay	ec50	0.0002	uM
1-[(3R)-1-[4-[2-[methyl(methylsulfonyl)amino]phenyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2127414: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin -induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0002	uM
1-[(3R)-1-[2,3-difluoro-4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl]-2-oxopyrrolidin-3-yl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]urea	2270773: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin-induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0002	uM
1-[(3R)-1-[4-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2264869: Agonist activity at human FPR2 receptor expressed in CHO cells assessed as forskolin/IBMX-induced intracellular cAMP level incubated for 30 mins by HTRF HiRange cAMP assay	ec50	0.0002	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(3-methyl-1,2-thiazol-5-yl)urea	1720303: Agonist activity at human FPR2 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	0.0003	uM
1-(5-chlorothiophen-2-yl)-3-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]urea	1720303: Agonist activity at human FPR2 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	0.0003	uM
1-(4-chlorophenyl)-3-[(1S)-1-[2-(2-hydroxyethyl)tetrazol-5-yl]-2-(4-methoxyphenyl)ethyl]urea	1932219: Agonist activity at human FPR2 expressed in HEK293 cells assessed as increase in calcium flux incubated for 45 mins by Fluo-4 AM dye based fluorescence assay	ec50	0.0003	uM
1-(4-fluorophenyl)-3-[(7R,8S)-7-(4-methoxyphenyl)-4-oxo-7,8-dihydro-6H-pyrrolo[2,1-c][1,2,4]oxadiazin-8-yl]urea	1932218: Agonist activity at FPR2 (unknown origin) assessed as increase in calcium flux	ec50	0.0003	uM
1-(4-fluorophenyl)-3-[(3R,4S)-4-(4-methoxyphenyl)oxolan-3-yl]urea	1731419: Agonist activity at FPR2 (unknown origin) by calcium mobilization assay	ec50	0.0003	uM
1-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-(4-methoxyphenyl)urea	2127414: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin -induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0003	uM
1-[(3R,4S)-3-(2,6-difluoro-4-methoxyphenyl)-5-(2-hydroxyethoxyamino)-3,4-dihydro-2H-pyrrol-4-yl]-3-(4-methoxyphenyl)urea	1932219: Agonist activity at human FPR2 expressed in HEK293 cells assessed as increase in calcium flux incubated for 45 mins by Fluo-4 AM dye based fluorescence assay	ec50	0.0003	uM
1-(4-chlorophenyl)-3-[(3R,4S)-4-(4-methoxyphenyl)-2-oxooxolan-3-yl]urea	2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay	ec50	0.0003	uM
(2-methylphenyl)methyl N-[2-(5-oxohexyl)-1,3-oxazol-4-yl]carbamate	2083663: Agonist activity at FPR2 (unknown origin) in HEK293 cells	ec50	0.0003	uM
1-(4-chlorophenyl)-3-[1-[2,3-difluoro-4-[(3R)-3-[2-hydroxyethyl(methyl)amino]pyrrolidin-1-yl]phenyl]-2-oxopyrrolidin-3-yl]urea	2264869: Agonist activity at human FPR2 receptor expressed in CHO cells assessed as forskolin/IBMX-induced intracellular cAMP level incubated for 30 mins by HTRF HiRange cAMP assay	ec50	0.0003	uM
1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[2,3-difluoro-4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl]-2-oxopyrrolidin-3-yl]urea	2270773: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin-induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0003	uM
1-[(3S,4R)-4-(3-fluoro-5-methoxy-2-pyridinyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1720303: Agonist activity at human FPR2 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	0.0004	uM
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-phenylurea	1720303: Agonist activity at human FPR2 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	0.0004	uM
1-[(3S,4R)-4-(2-fluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-(4-fluorophenyl)urea	1720303: Agonist activity at human FPR2 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	0.0004	uM
2-piperidin-4-ylethyl (2R,3R)-3-[(6-bromo-3-pyridinyl)carbamoyl]spiro[bicyclo[2.2.1]heptane-7,1’-cyclopropane]-2-carboxylate	2083663: Agonist activity at FPR2 (unknown origin) in HEK293 cells	ec50	0.0004	uM
1-[(3R)-1-[2,3-difluoro-4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2127414: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin -induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0004	uM
N-[[1-[4-[(3R)-3-[(4-chloro-2-fluorophenyl)carbamoylamino]-2-oxopyrrolidin-1-yl]-2,3-difluorophenyl]cyclopropyl]methyl]acetamide	2270773: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin-induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0004	uM
1-[(3R)-1-[4-[2-(tert-butylsulfamoyl)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-[4-(trifluoromethyl)phenyl]urea	2127414: Agonist activity at human FPR2 expressed in CHO cells assessed as forskolin -induced cAMP level incubated for 30 mins in presence of IBMX by HTRF HiRange cAMP assay	ec50	0.0005	uM

CTD chemical–gene interactions

24 total (human), top 24 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
lipoxin A4	affects binding, decreases activity, increases activity, increases abundance, increases expression	2
Air Pollutants, Occupational	affects expression, decreases expression	2
triphenyl phosphate	affects expression	1
sulforaphane	increases expression	1
cobaltous chloride	increases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	affects binding, increases reaction	1
nordy	decreases expression	1
gardiquimod	increases expression, decreases reaction	1
Air Pollutants	increases abundance, increases expression	1
Arsenic	affects methylation	1
Aspirin	increases expression, increases abundance	1
Benzo(a)pyrene	increases methylation	1
Cisplatin	increases expression	1
Methotrexate	decreases expression	1
Nickel	decreases expression	1
Ozone	increases abundance, increases expression	1
Quercetin	increases expression	1
Tetrachlorodibenzodioxin	decreases expression	1
Tretinoin	increases expression	1
Cyclosporine	increases methylation	1
Aflatoxin B1	increases methylation	1
Antirheumatic Agents	decreases expression	1
Protein Kinase Inhibitors	decreases reaction, increases expression	1

ChEMBL screening assays

194 unique, capped per target: 110 binding, 84 functional

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

7 cell lines: 4 spontaneously immortalized cell line, 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_A6US	NP-2/CD4/FPRL1	Cancer cell line	Male
CVCL_F1U0	HyCyte THP-1 KO-hFPR2	Cancer cell line	Male
CVCL_H432	CHO-K1/FPRL1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV17	cAMP Hunter CHO-K1 FPRL1 Gi	Spontaneously immortalized cell line	Female
CVCL_KX06	PathHunter CHO-K1 FPRL1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA32	PathHunter U2OS FPRL1 Activated GPCR Internalization	Cancer cell line	Female
CVCL_ZK57	GeneBLAzer FPRL-1-Galpha15-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

showing 60 of 295 trials:

NCT	Phase	Status	Title
NCT00417066	Phase 4	COMPLETED	Flexible GnRH Antagonist vs Flare up GnRH Agonist Protocol in Poor Responders
NCT00732693	Phase 4	COMPLETED	Evaluation of Physiologic and Standard Sex Steroid Replacement Regimens in Women With Premature Ovarian Failure
NCT00837616	Phase 4	COMPLETED	Estrogen Dosing in Turner Syndrome: Pharmacology and Metabolism
NCT01853501	Phase 4	UNKNOWN	Effects of ADSC Therapy in Women With POF
NCT02783937	Phase 4	COMPLETED	Filgrastim for Premature Ovarian Insufficiency
NCT03535480	Phase 4	UNKNOWN	Autologous Bone Marrow Stem Cell Ovarian Transplantation to Restore Ovarian Function in Premature Ovarian Failure
NCT02399566	Phase 4	UNKNOWN	Clinical Trial of Erlotinib and Pemetrexed for Maintenance Treatment in Lung Adenocarcinoma
NCT02804646	Phase 4	UNKNOWN	Endostar Durative Transfusion Combined With Chemotherapy in the Treatment of Advanced Lung Adenocarcinoma
NCT00140998	Phase 3	COMPLETED	Estrogen Treatment (Oral vs. Patches) in Turner Syndrome
NCT00002852	Phase 3	COMPLETED	Surgery With or Without Chemotherapy in Treating Patients With Stage I Non-small Cell Lung Cancer
NCT00005838	Phase 3	COMPLETED	Combination Chemotherapy Plus Radiation Therapy With or Without AE-941 in Treating Patients With Stage III Non-small Cell Lung Cancer That Cannot Be Removed By Surgery
NCT00020709	Phase 3	COMPLETED	Combination Chemotherapy and Radiation Therapy With or Without Gefitinib in Treating Patients With Stage III Non-Small Cell Lung Cancer That Cannot Be Removed By Surgery
NCT00049543	Phase 3	COMPLETED	Gefitinib in Treating Patients With Stage IB, II, or IIIA Non-small Cell Lung Cancer That Was Completely Removed by Surgery
NCT00946712	Phase 3	TERMINATED	S0819: Carboplatin and Paclitaxel With or Without Bevacizumab and/or Cetuximab in Treating Patients With Stage IV or Recurrent Non-Small Cell Lung Cancer
NCT01798485	Phase 3	TERMINATED	A Phase 3 Study of Ganetespib in Combination With Docetaxel Versus Docetaxel Alone in Patients With Advanced NSCLC
NCT02011997	Phase 3	UNKNOWN	Comparison of cVATS Segmentectomy Versus Lobectomy for Lung Adenocarcinoma in Situ and With Microinvasion
NCT03391869	Phase 3	ACTIVE_NOT_RECRUITING	Nivolumab and Ipilimumab With or Without Local Consolidation Therapy in Treating Patients With Stage IV Non-Small Cell Lung Cancer
NCT03676192	Phase 3	COMPLETED	To Compare Efficacy and Safety of CT-P16 and European Union-Approved Avastin as First-Line Treatment for Metastatic or Recurrent Non-Squamous Non-Small Cell Lung Cancer
NCT04339218	Phase 3	RECRUITING	Cryoablation in Combination (or Not) With Pembrolizumab and Pemetrexed-carboplatin in 1st-line Treatment for Patients With Metastatic Lung Adenocarcinoma
NCT05204758	Phase 3	COMPLETED	Prophylactic TCM for Mitigation of EGFR-TKI Related Dermatological Adverse Effect
NCT05717803	Phase 3	RECRUITING	Segmentectomy for Ground Glass-dominant Invasive Lung Cancer (ECTOP-1012)
NCT05943795	Phase 3	ACTIVE_NOT_RECRUITING	A Clinical Study of SI-B001 Combined With Docetaxel in the Treatment of Non-small Cell Lung Adenocarcinoma and Lung Squamous Cell Carcinoma
NCT06031181	Phase 3	RECRUITING	Sublobar Resection for Adenocarcinoma in Situ/Minimally Invasive Adenocarcinoma Diagnosed by Intraoperative Frozen Section (ECTOP-1019)
NCT06031246	Phase 3	RECRUITING	Selective Lymph Node Dissection for cT1N0M0 Invasive NSCLC With CTR>0.5 Located in the Apical Segment (ECTOP-1018)
NCT06634966	Phase 3	RECRUITING	Segmentectomy for Solid-dominant Lung Cancer
NCT07169903	Phase 3	NOT_YET_RECRUITING	Segmentectomy vs Lobectomy for 2 - 3cm IASLC Grade 1-2 Lung Adenocarcinoma: A Multi-center RCT
NCT07481786	Phase 3	RECRUITING	Bevacizumab Plus FSRT Versus Hippocampus-Avoidant WBRT in Lung Adenocarcinoma With Extensive Brain Metastases
NCT00001951	Phase 2	COMPLETED	Hormone Replacement in Young Women With Premature Ovarian Failure
NCT00370019	Phase 2	WITHDRAWN	Effects of an Estrogen Replacement Therapy Skin Patch on Ovulation in Women With Premature Ovarian Failure
NCT00429494	Phase 2	COMPLETED	GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients
NCT03816852	Phase 2	SUSPENDED	The Safety and Efficiency Study of Mesenchymal Stem Cell (19#iSCLife®-POI) in Premature Ovarian Insufficiency
NCT04536467	Phase 2	UNKNOWN	Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients
NCT06117982	Phase 2	COMPLETED	The Impact of Granulocyte Colony Stimulating Factor on Premature Ovarian Insufficiency
NCT00040794	Phase 2	COMPLETED	Combination Chemotherapy, Radiation Therapy, and Gefitinib in Treating Patients With Stage III Non-Small Cell Lung Cancer
NCT00087412	Phase 2	COMPLETED	S0341: Erlotinib in Treating Patients With Advanced Primary Non-Small Cell Lung Cancer
NCT00118144	Phase 2	COMPLETED	Bortezomib in Treating Patients With Stage IIIB or Stage IV Lung Cancer
NCT00118183	Phase 2	COMPLETED	Docetaxel With Either Cetuximab or Bortezomib as First-Line Therapy in Treating Patients With Stage III or Stage IV Non-Small Cell Lung Cancer
NCT00126581	Phase 2	COMPLETED	Erlotinib Hydrochloride With or Without Carboplatin and Paclitaxel in Treating Patients With Stage III-IV Non-small Cell Lung Cancer
NCT00334815	Phase 2	ACTIVE_NOT_RECRUITING	Combination Chemotherapy, Radiation Therapy, and Bevacizumab in Treating Patients With Newly Diagnosed Stage III Non-small Cell Lung Cancer That Cannot Be Removed by Surgery
NCT00368992	Phase 2	COMPLETED	S0536: Cetuximab, Paclitaxel, Carboplatin, and Bevacizumab in Treating Patients With Advanced Non-Small Cell Lung Cancer
NCT00511485	Phase 2	COMPLETED	Study of Vintafolide (MK-8109, EC145) in Participants With Progressive Adenocarcinoma of the Lung (MK-8109-008, EC-FV-03)
NCT00950365	Phase 2	COMPLETED	Pemetrexed Disodium With or Without Erlotinib Hydrochloride in Treating Patients With Stage IIIB-IV or Recurrent Non-Small Cell Lung Cancer
NCT00955305	Phase 2	TERMINATED	Paclitaxel, Carboplatin, and Bevacizumab With or Without Cixutumumab in Treating Patients With Stage IV or Recurrent Non-small Cell Lung Cancer
NCT01218516	Phase 2	COMPLETED	A Safety and Efficacy Study of Farletuzumab in Participants With Adenocarcinoma of the Lung
NCT01294306	Phase 2	COMPLETED	MK2206 and Erlotinib Hydrochloride in Treating Patients With Advanced Non-Small Cell Lung Cancer Who Have Progressed After Previous Response to Erlotinib Hydrochloride Therapy
NCT01557959	Phase 2	COMPLETED	Docetaxel, Cisplatin, Pegfilgrastim, and Erlotinib Hydrochloride in Treating Patients With Stage IIIB or Stage IV Non-Small Cell Lung Cancer
NCT01561456	Phase 2	COMPLETED	Study of AXL1717 Compared to Docetaxel to Treat Squamous Cell Carcinoma or Adenocarcinoma of the Lung
NCT01578551	Phase 2	TERMINATED	Study of Metformin Plus Paclitaxel/Carboplatin/Bevacizumab in Patients With Adenocarcinoma.
NCT01578668	Phase 2	COMPLETED	Erlotinib Plus Pemetrexed to Treat Lung Adenocarcinoma With Brain Metastases
NCT01819428	Phase 2	TERMINATED	NOV120101 (Poziotinib) for 1st Line Monotherapy in Patients With Lung Adenocarcinoma
NCT01935336	Phase 2	COMPLETED	Study of Ponatinib in Patients With Lung Cancer Preselected Using Different Candidate Predictive Biomarkers
NCT02134912	Phase 2	TERMINATED	S1300: Pemetrexed Disodium With or Without Crizotinib in Treating Patients With Stage IV Non-Small Cell Lung Cancer That Has Progressed After Crizotinib
NCT02186847	Phase 2	COMPLETED	Chemotherapy and Radiation Therapy With or Without Metformin Hydrochloride in Treating Patients With Stage III Non-small Cell Lung Cancer
NCT02264210	Phase 2	COMPLETED	Icotinib for Completed Resected IB NSCLC With EGFR Mutation
NCT02493582	Phase 2	ACTIVE_NOT_RECRUITING	The Study of Apatinib Plus CIK as the Third Line Therapy for Advanced Lung Adenocarcinoma Patients With Wild-Type EGFR
NCT02621333	Phase 2	TERMINATED	Chemotherapy Combined Autologous Cytokine-induced Killer Cells in Naive Stage IV EGFR-wild Type Lung Adenocarcinoma
NCT02737774	Phase 2	UNKNOWN	Alternating Icotinib and Chemotherapy for Advanced Non-small Cell Lung Cancer With EGFR Mutation
NCT02759835	Phase 2	COMPLETED	Local Ablative Therapy for Treatment of Oligoprogressive, EGFR-Mutated, Non-Small Cell Lung Cancer After Treatment With Osimertinib
NCT02787447	Phase 2	UNKNOWN	Radiotherapy Combined With Thymosin for Metastatic NSCLC Patients Who Showed Stable Disease After First Line TKI Therapy
NCT02788058	Phase 2	UNKNOWN	A Study of Hypofractionated Radiotherapy for Limited Metastatic NSCLC Harboring Sensitizing EGFR Mutations After First Line TKI Therapy

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for FPR2 across ~30M SureChEMBL compounds — explore on Sugi Predict.