FPR2
geneOn this page
Also known as LXA4RHM63FPRH2FMLPXFPR2AFMLP-R-IIALXRALX
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 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 48 total
- Druggable target: yes — 4 molecules with ChEMBL bioactivity
- 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: 6 — 6 protein_coding
ENST00000340023, ENST00000598776, ENST00000598953, ENST00000599326, ENST00000600258, ENST00000600722
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.
FANTOM5 promoters (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
284 total, 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 |
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 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): BHLHA15, CREBZF, TAL1
miRNA regulators (miRDB)
47 targeting FPR2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-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 |
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)
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 (51 total): helix 18, topological domain 8, transmembrane region 7, strand 6, binding site 3, turn 3, chain 1, region of interest 1, compositionally biased region 1, glycosylation site 1, disulfide bond 1, sequence conflict 1
Structure
Experimental structures (PDB)
13 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8ZBW | ELECTRON MICROSCOPY | 2.58 |
| 6LW5 | X-RAY DIFFRACTION | 2.8 |
| 7WVX | ELECTRON MICROSCOPY | 2.8 |
| 7T6U | ELECTRON MICROSCOPY | 2.9 |
| 7WVV | ELECTRON MICROSCOPY | 2.9 |
| 7T6S | ELECTRON MICROSCOPY | 3 |
| 7WVY | ELECTRON MICROSCOPY | 3 |
| 7T6V | ELECTRON MICROSCOPY | 3.1 |
| 7WVW | ELECTRON MICROSCOPY | 3.1 |
| 6OMM | ELECTRON MICROSCOPY | 3.17 |
| 8Y62 | ELECTRON MICROSCOPY | 3.2 |
| 8Y63 | ELECTRON MICROSCOPY | 3.2 |
| 9JHJ | ELECTRON MICROSCOPY | 3.2 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P25090-F1 | 84.87 | 0.66 |
Antibody-complex structures (SAbDab): 6 — 6OMM, 7T6S, 7T6U, 7T6V, 8Y62, 9JHJ
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): 106; 201; 205
Disulfide bonds (1): 98–176
Glycosylation sites (1): 4
Function
Pathways and Gene Ontology
Reactome pathways
4 pathways
| ID | Pathway |
|---|---|
| R-HSA-416476 | G alpha (q) signalling events |
| R-HSA-418594 | G alpha (i) signalling events |
| R-HSA-444473 | Formyl peptide receptors bind formyl peptides and many other ligands |
| R-HSA-6798695 | Neutrophil degranulation |
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 (29): 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), negative regulation of neuron apoptotic process (GO:0043524), 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), 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
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| GPCR downstream signalling | 2 |
| Peptide ligand-binding receptors | 1 |
| Innate Immune System | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| secretory granule membrane | 3 |
| glial cell activation | 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 |
| negative regulation of apoptotic process | 1 |
| regulation of neuron apoptotic process | 1 |
| neuron apoptotic process | 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 |
Protein interactions and networks
STRING
1792 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| FPR2 | ANXA1 | P04083 | 999 |
| FPR2 | CAMP | P49913 | 997 |
| FPR2 | HSH2D | Q96JZ2 | 845 |
| FPR2 | PLAUR | Q03405 | 790 |
| FPR2 | APP | P05067 | 759 |
| FPR2 | TRIM11 | Q96F44 | 683 |
| FPR2 | SAA1 | P02735 | 683 |
| FPR2 | PRNP | P04156 | 675 |
| FPR2 | A0A087WTN9 | A0A087WTN9 | 672 |
| FPR2 | PLEKHF1 | Q96S99 | 653 |
| FPR2 | ITGAM | P11215 | 623 |
| FPR2 | RARRES2 | Q99969 | 622 |
| FPR2 | SCARB1 | Q8WTV0 | 610 |
| FPR2 | CXCL1 | P09341 | 602 |
| FPR2 | IL27RA | Q6UWB1 | 595 |
IntAct
23 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| FPR2 | ARL6IP5 | psi-mi:“MI:0914”(association) | 0.640 |
| APOD | FPR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FPR2 | FXYD6 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FPR2 | LRRC25 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FPR2 | SSMEM1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| APP | FPR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FPR2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| FPR2 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | FPR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| FPR2 | GPR89A | psi-mi:“MI:0914”(association) | 0.350 |
| FPR2 | SCAMP3 | psi-mi:“MI:0914”(association) | 0.350 |
| FXYD6 | FPR2 | psi-mi:“MI:0915”(physical association) | 0.000 |
| FPR2 | LRRC25 | psi-mi:“MI:0915”(physical association) | 0.000 |
| FPR2 | SSMEM1 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (197): FUNDC2 (Affinity Capture-MS), REEP6 (Affinity Capture-MS), ATP2B3 (Affinity Capture-MS), SLC38A9 (Affinity Capture-MS), FNDC3A (Affinity Capture-MS), SLC30A5 (Affinity Capture-MS), RRAGB (Affinity Capture-MS), ELOVL2 (Affinity Capture-MS), ATP2B4 (Affinity Capture-MS), DOLK (Affinity Capture-MS), ARL6IP1 (Affinity Capture-MS), RTN2 (Affinity Capture-MS), CERS5 (Affinity Capture-MS), TRIM4 (Affinity Capture-MS), CAMLG (Affinity Capture-MS)
ESM2 similar proteins: A4FUQ5, B9VR26, O08790, O35786, O70129, O75388, O88416, O88536, O88537, O97664, P0C7U4, P21462, P21730, P25089, P25090, P30992, P30993, P33766, P35343, P35407, P46090, P46091, P79175, P79176, P79177, P79178, P79188, P79189, P79190, P79191, P79234, P79235, P79236, P79237, P79240, P79241, P79242, P79243, P97468, P97520
Diamond homologs: A4FUQ5, B1PHQ8, B9VR26, O08565, O08790, O35210, O35786, O62747, O70129, O75388, O77590, O88416, O88536, O88537, O97571, O97664, P0C7U4, P0C7U5, P21462, P21730, P25025, P25089, P25090, P25095, P25104, P28646, P29089, P29754, P29755, P30555, P30556, P30872, P30873, P30937, P30992, P30993, P31391, P33766, P34976, P35373
SIGNOR signaling
5 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 |
Disease & clinical
Clinical variants and AI predictions
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 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
236 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:51761227:GCTG:G | donor_gain | 0.9800 |
| 19:51763442:A:G | donor_gain | 0.9800 |
| 19:51768638:GTTTC:G | acceptor_loss | 0.9800 |
| 19:51768639:TTTCA:T | acceptor_loss | 0.9800 |
| 19:51768640:TTCAG:T | acceptor_loss | 0.9800 |
| 19:51768641:TCAGG:T | acceptor_loss | 0.9800 |
| 19:51768642:CAGGT:C | acceptor_loss | 0.9800 |
| 19:51768643:A:AG | acceptor_gain | 0.9800 |
| 19:51768643:A:T | acceptor_loss | 0.9800 |
| 19:51768644:G:GG | acceptor_gain | 0.9800 |
| 19:51761228:CTGG:C | donor_loss | 0.9700 |
| 19:51761229:TGG:T | donor_loss | 0.9700 |
| 19:51761230:GGTAA:G | donor_loss | 0.9700 |
| 19:51761231:G:GG | donor_gain | 0.9700 |
| 19:51761231:GTAAG:G | donor_loss | 0.9700 |
| 19:51761232:T:A | donor_loss | 0.9700 |
| 19:51768644:GGT:G | acceptor_gain | 0.9700 |
| 19:51761228:CTG:C | donor_gain | 0.9300 |
| 19:51763488:GTCA:G | donor_gain | 0.9300 |
| 19:51763489:TCAT:T | donor_gain | 0.9300 |
| 19:51761011:TG:T | donor_gain | 0.9200 |
| 19:51761226:TGCTG:T | donor_gain | 0.9100 |
| 19:51761227:GCTGG:G | donor_gain | 0.9100 |
| 19:51761212:A:T | donor_gain | 0.8900 |
| 19:51761233:AA:A | donor_loss | 0.8900 |
| 19:51768637:T:TA | acceptor_gain | 0.8800 |
| 19:51761229:TG:T | donor_gain | 0.8700 |
| 19:51761230:GG:G | donor_gain | 0.8700 |
| 19:51761013:AAG:A | donor_gain | 0.8600 |
| 19:51767350:C:T | donor_gain | 0.8100 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000288991 (19:51767826 G>A,T), RS1000301661 (19:51761236 T>C,G), RS1000806940 (19:51768099 T>G), RS1000822672 (19:51764003 C>T), RS1001178751 (19:51760241 T>C), RS1001295458 (19:51760528 T>C), RS1001628880 (19:51761829 G>A), RS1001664588 (19:51764980 C>T), RS1001741533 (19:51762223 T>C), RS1001820156 (19:51765560 G>A), RS1001968450 (19:51768519 G>T), RS1002123165 (19:51768302 C>A,T), RS1002301745 (19:51761683 C>T), RS1002571711 (19:51769976 G>A), RS1002631542 (19:51763146 A>G,T)
Disease associations
OMIM: gene MIM:136538 | disease phenotypes:
GenCC curated gene-disease
Mondo (2): primary ovarian failure (MONDO:0005387), lung adenocarcinoma (MONDO:0005061)
Orphanet (2): NON RARE IN EUROPE: Primary ovarian failure (Orphanet:619), NON RARE IN EUROPE: Adenocarcinoma of the lung (Orphanet:415268)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004866_7 | Alopecia areata | 6.000000e-06 |
| GCST005531_84 | Multiple sclerosis | 3.000000e-06 |
| GCST007277_24 | Tourette syndrome | 9.000000e-07 |
| GCST009597_232 | Multiple sclerosis | 2.000000e-06 |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D016649 | Primary Ovarian Insufficiency | C12.050.351.500.056.630.750; C12.100.250.056.630.750; C19.391.630.750 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL3038479 (PROTEIN FAMILY), CHEMBL4227 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 79,620 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4 | 59,532 |
| CHEMBL422 | TRIFLUOPERAZINE | 4 | 20,044 |
| CHEMBL6056273 | IDREBORMILAST | 2 | 19 |
| CHEMBL4784510 | BMS-986235 | 1 | 25 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Formylpeptide receptors
Most potent curated ligand interactions (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)
344 measured of 687 human assays (700 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| MLS000079917 | EC50 | 0.0133 nM | |
| 2-(3-chlorophenyl)-4-N-methyltriazole-4,5-diamine | EC50 | 0.325 nM | |
| 3-[(4- iodophenyl)carbamoyl] spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-2-carboxylic acid | EC50 | 0.6 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 4-chloro-N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-1-[4-methoxy-6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]-2-pyridinyl]-2-oxopyrrolidin-3-yl]benzamide | EC50 | 0.6 nM | US-20230348426: OXOPYRROLIDINE FPR2 AGONISTS |
| 1-(4-bromophenyl)-3-{4-[2-(2- hydroxyphenyl)ethyl]-4- methyl-2,5-dioxoimidazolidin- 1-yl}urea | EC50 | 0.97 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(2S)-2-{[(4- bromophenyl)carbamoyl]amino}- 4-methylpentanoyl]amino} pentanoic acid | EC50 | 1 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 3-({[-{[(4-bromo-2- fluorophenyl)carbamoyl]amino}- 2,5-dioxo-4-(propan-2- yl)imidazolidin-4- yl]acetyl}amino)propanoic acid | EC50 | 1 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-N-(2-amino-2-oxoethyl)- 2-{[(4- bromophenyl)carbamoyl]amino}- 4-methylpentanamide | EC50 | 1.1 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| {[2-{[(4- bromophenyl)carbamoyl] amino}-3-(1H-indol-3- yl)propanoyl]amino}acetic acid | EC50 | 1.4 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 3-[(4- iodophenyl)carbamoyl] spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-5-ene-2- carboxylic acid | EC50 | 1.6 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| N-(4-iodophenyl) spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-5-ene-2,3- dicarboxamide | EC50 | 1.6 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 3-[(4- iodophenyl)carbamoyl]-7,7- dimethylbicyclo[2.2.1]heptane- 2-carboxylic acid | EC50 | 1.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(2S)-2-{[(4- bromophenyl)carbamoyl]amino}- 4-methylpentanoyl]amino}-3- methylbutanoic acid | EC50 | 1.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- bromophenyl)carbamoyl]amino}- N-[2-(dimethylamino)-2- oxoethyl]-4- methylpentanamide | EC50 | 1.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| {[(2S)-4-methyl-2-({[4- (trifluoromethyl)phenyl] carbamoyl}amino)pentanoyl] amino}acetic acid | EC50 | 1.8 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| N-(4-iodophenyl) spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-2,3- dicarboxamide | EC50 | 1.9 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| {[(2S)-2-{[(4- bromophenyl)carbamoyl] amino}4- methylpentanoyl]amino} methanesulfonic acid | EC50 | 2 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromophenyl)-3-{4-[2-(3- hydroxyphenyl)ethyl]-4- methyl-2,5-dioxoimidazolidin- 1-yl}urea | EC50 | 2.1 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromo-2-fluorophenyl)- 3-{4-[2-(3- hydroxyphenyl)ethyl]-4- methyl-2,5-dioxoimidazolidin- 1-yl}urea | EC50 | 2.2 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- bromophenyl)carbamoyl]amino}- 4-methyl-N-(1H-tetrazol- 5-ylmethyl)pentanamide | EC50 | 2.3 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-[2-(3-aminopropyl)-3-(4- cyanophenyl)-1-oxo-1,2,3,4- tetrahydroisoquinolin-7-yl]-3- [4-(methylsulfanyl)phenyl]urea | EC50 | 2.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| N-(4-bromophenyl) spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-2,3- dicarboxamide | EC50 | 2.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-N-(2-amino-2-oxoethyl)- 2-{[(4- bromophenyl)carbamoyl]amino} pentanamide | EC50 | 2.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- bromophenyl)carbamoyl]amino}- N-(2-hydroxy-2- methylpropyl)-4- methylpentanamide | EC50 | 2.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 2-methyl-2-{[(2S)-4-methyl-2-({[4- (trifluoromethyl)phenyl]carbamoyl} amino)pentanoyl]amino} propanoic acid | EC50 | 2.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| N-(4-iodophenyl)-7,7- dimethylbicyclo[2.2.1]heptane- 2,3-dicarboxamide | EC50 | 2.6 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 2-[1-{[(4- bromophenyl)carbamoyl]amino}- 2,5-dioxo-4-(propan-2- yl)imidazolidin-4-yl]-N-(2- hydroxyethyl)acetamide | EC50 | 2.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| CHEMBL4747556 | EC50 | 2.9 nM | |
| (2S)-2-{[(4- bromophenyl)carbamoyl]amino}- N-[(2R)-1- hydroxypropan-2-yl]-4- methylpentanamide | EC50 | 3 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2-{(1S)-2-Methyl-1- [({[4- (trifluoromethyl)phenyl] amino}carbonyl)amino] propyl}-1H-imidazol-1- yl)acetic acid | EC50 | 3 nM | US-10301269: Imidazole derivatives as formyl peptide receptor modulators |
| 1-(4-bromophenyl)-3-[4- methyl-2,5-dioxo-4-(2- phenylethyl)imidazolidin-1- yl]urea | EC50 | 3.2 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromophenyl)-3-[4-ethyl- 2,5-dioxo-4-(propan-2- yl)imidazolidin-1-yl]urea | EC50 | 3.3 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromophenyl)-3-{4- methyl-4-[2-(5-methylfuran-2- yl)ethyl]-2,5- dioxoimidazolidin-1-yl}urea | EC50 | 3.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-4-methyl-N-(1H-tetrazol- 5-ylmethyl)-2-({[4- (trifluoromethyl)phenyl]carbamoyl} amino)pentanamide | EC50 | 3.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromophenyl)-3-[2,5- dioxo-4,4-di(propan-2- yl)imidazolidin-1-yl]urea | EC50 | 3.8 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 3-({[1-{[(4- bromophenyl)carbamoyl]amino}- 2,5-dioxo-4-(propan-2- yl)imidazolidin-4- yl]acetyl}amino)propanoic acid | EC50 | 3.9 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 3-[(4- bromophenyl)carbamoyl] spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-5-ene-2- carboxylic acid | EC50 | 4 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromo-2-fluorophenyl)- 3-{4-[2-(2- hydroxyphenyl)ethyl]-4- methyl-2,5-dioxoimidazolidin- 1-yl}urea | EC50 | 4 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- iodophenyl)carbamoyl]amino}- 4-methylpentanoic acid | EC50 | 4 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-[(1S)-1-(1H-imidazol- 2-yl)-2-methylpropyl]- 3-[4- (trifluoromethyl)phenyl] urea | EC50 | 4 nM | US-10301269: Imidazole derivatives as formyl peptide receptor modulators |
| rel-(2R,3S)-3-[(4- bromophenyl)carbamoyl]spiro [bicyclo[2.2.1]heptane-7,1’- cyclopropane]-2-carboxylic acid | EC50 | 4 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-N-(2-amino-2-oxoethyl)- 2-{[(4-bromo-2- fluorophenyl)carbamoyl]amino}- 4-methylpentanamide | EC50 | 4.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S,3S)-N-(2-amino-2- oxoethyl)-2-{[(4- bromophenyl)carbamoyl]amino}- 3-methylpentanamide | EC50 | 4.6 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- bromophenyl)carbamoyl]amino}- 4-methyl-N-(2- oxopropyl)pentanamide | EC50 | 4.7 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| N-(4-bromophenyl) spiro[bicyclo[2.2.1]heptane- 7,1’-cyclopropane]-5-ene-2,3- dicarboxamide | EC50 | 4.8 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-2-{[(4- bromophenyl)carbamoyl] amino}-N-(2,3-dihydroxypropyl)- 4-methylpentanamide | EC50 | 5.1 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-(4-bromophenyl)-3-{4-[2- (furan-2-yl)ethyl]-4-methyl- 2,5-dioxoimidazolidin-1- yl}urea | EC50 | 5.2 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-N-(2-amino-2-oxoethyl)- 2-{[(4-bromo-2- fluorophenyl)carbamoyl]amino} pentanamide | EC50 | 5.2 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| 1-{3-(4-cyanophenyl)-2-[2- (1H-imidazol-4-yl)ethyl]-1- oxo-1,2,3,4- tetrahydroisoquinolin-7-yl}-3- [4-(methylsulfanyl)phenyl]urea | EC50 | 5.5 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
| (2S)-N-[(2S)-1-amino-3- methyl-1-oxobutan-2-yl]-2- {[(4- bromophenyl)carbamoyl]amino}- 4-methylpentanamide | EC50 | 5.8 nM | US-10434112: Use of agonists of formyl peptide receptor 2 for treating dermatological diseases |
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
711 with measured affinity, of 1689 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-(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 |
| (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-[(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-[(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-[(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 |
| 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 |
| 1-[(3R)-1-[4-[2-(tert-butylsulfamoyl)phenyl]phenyl]-2-oxopiperidin-3-yl]-3-(4-chlorophenyl)urea | 2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay | ec50 | 0.0005 | uM |
| 1-(4-chloro-2-fluorophenyl)-3-[(3R)-1-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-2-oxopyrrolidin-3-yl]urea | 2083657: Agonist activity at FPR2 (unknown origin) expressed in CHO cells by cAMP assay | ec50 | 0.0005 | uM |
| 1-(4-chloro-2-fluorophenyl)-3-[(7R)-5-[4-(2-dimethylphosphorylphenyl)-2,3-difluorophenyl]-6-oxo-5-azaspiro[2.4]heptan-7-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 | 0.0005 | uM |
| methyl (E,5S,6R)-5,6-dihydroxy-8-[5-[(1R)-1-hydroxyhexyl]-2,3-diphenylimidazol-4-yl]oct-7-enoate | 1585252: 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-6 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay | ic50 | 0.0005 | uM |
| 1-(4-bromophenyl)-3-[4-ethyl-2,5-dioxo-4-(2-phenylethyl)imidazolidin-1-yl]urea | 2083637: Agonist activity at human FPR2 expressed in HL-60 cells assessed as inhibition of WKYMVM-induced calcium mobilization | ec50 | 0.0005 | uM |
| N-(4-bromophenyl)-2-(4-ethyl-2,5-dioxo-4-propan-2-ylimidazolidin-1-yl)acetamide | 2083649: Agonist activity at human FPR2 expressed in CHO cells assessed as increase in calcium mobilization by Fluo-4 AM dye based fluorescence assay | ec50 | 0.0005 | uM |
| 1-(4-chlorophenyl)-3-[(1S)-2-(4-ethylphenyl)-1-[5-[2-hydroxyethyl(methyl)amino]-1,2,4-oxadiazol-3-yl]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 | 0.0006 | uM |
| 1-[(1Z,2S)-1-amino-3-(4-ethylphenyl)-1-(2-hydroxyethoxyimino)propan-2-yl]-3-(4-chlorophenyl)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 | 0.0006 | uM |
| 1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-[(3R)-1-[4-[2-(methanesulfonamido)phenyl]phenyl]-2-oxopiperidin-3-yl]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 | 0.0006 | uM |
CTD chemical–gene interactions
22 total (human), top 22 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| lipoxin A4 | increases expression, affects binding, decreases activity, increases activity, increases abundance | 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 |
| Arsenic | affects methylation | 1 |
| Aspirin | increases abundance, increases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Cisplatin | increases expression | 1 |
| Methotrexate | decreases expression | 1 |
| Nickel | decreases 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)
289 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00417066 | PHASE4 | COMPLETED | Flexible GnRH Antagonist vs Flare up GnRH Agonist Protocol in Poor Responders |
| NCT00732693 | PHASE4 | COMPLETED | Evaluation of Physiologic and Standard Sex Steroid Replacement Regimens in Women With Premature Ovarian Failure |
| NCT00837616 | PHASE4 | COMPLETED | Estrogen Dosing in Turner Syndrome: Pharmacology and Metabolism |
| NCT01853501 | PHASE4 | UNKNOWN | Effects of ADSC Therapy in Women With POF |
| NCT02783937 | PHASE4 | COMPLETED | Filgrastim for Premature Ovarian Insufficiency |
| NCT03535480 | PHASE4 | UNKNOWN | Autologous Bone Marrow Stem Cell Ovarian Transplantation to Restore Ovarian Function in Premature Ovarian Failure |
| NCT02399566 | PHASE4 | UNKNOWN | Clinical Trial of Erlotinib and Pemetrexed for Maintenance Treatment in Lung Adenocarcinoma |
| NCT02804646 | PHASE4 | UNKNOWN | Endostar Durative Transfusion Combined With Chemotherapy in the Treatment of Advanced Lung Adenocarcinoma |
| NCT00140998 | PHASE3 | COMPLETED | Estrogen Treatment (Oral vs. Patches) in Turner Syndrome |
| NCT00002852 | PHASE3 | COMPLETED | Surgery With or Without Chemotherapy in Treating Patients With Stage I Non-small Cell Lung Cancer |
| NCT00005838 | PHASE3 | 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 | PHASE3 | 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 | PHASE3 | COMPLETED | Gefitinib in Treating Patients With Stage IB, II, or IIIA Non-small Cell Lung Cancer That Was Completely Removed by Surgery |
| NCT00946712 | PHASE3 | 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 | PHASE3 | TERMINATED | A Phase 3 Study of Ganetespib in Combination With Docetaxel Versus Docetaxel Alone in Patients With Advanced NSCLC |
| NCT02011997 | PHASE3 | UNKNOWN | Comparison of cVATS Segmentectomy Versus Lobectomy for Lung Adenocarcinoma in Situ and With Microinvasion |
| NCT03391869 | PHASE3 | ACTIVE_NOT_RECRUITING | Nivolumab and Ipilimumab With or Without Local Consolidation Therapy in Treating Patients With Stage IV Non-Small Cell Lung Cancer |
| NCT03676192 | PHASE3 | 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 | PHASE3 | RECRUITING | Cryoablation in Combination (or Not) With Pembrolizumab and Pemetrexed-carboplatin in 1st-line Treatment for Patients With Metastatic Lung Adenocarcinoma |
| NCT05204758 | PHASE3 | COMPLETED | Prophylactic TCM for Mitigation of EGFR-TKI Related Dermatological Adverse Effect |
| NCT05717803 | PHASE3 | RECRUITING | Segmentectomy for Ground Glass-dominant Invasive Lung Cancer (ECTOP-1012) |
| NCT05943795 | PHASE3 | 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 | PHASE3 | RECRUITING | Sublobar Resection for Adenocarcinoma in Situ/Minimally Invasive Adenocarcinoma Diagnosed by Intraoperative Frozen Section (ECTOP-1019) |
| NCT06031246 | PHASE3 | RECRUITING | Selective Lymph Node Dissection for cT1N0M0 Invasive NSCLC With CTR>0.5 Located in the Apical Segment (ECTOP-1018) |
| NCT06634966 | PHASE3 | RECRUITING | Segmentectomy for Solid-dominant Lung Cancer |
| NCT07169903 | PHASE3 | NOT_YET_RECRUITING | Segmentectomy vs Lobectomy for 2 - 3cm IASLC Grade 1-2 Lung Adenocarcinoma: A Multi-center RCT |
| NCT07481786 | PHASE3 | RECRUITING | Bevacizumab Plus FSRT Versus Hippocampus-Avoidant WBRT in Lung Adenocarcinoma With Extensive Brain Metastases |
| NCT00001951 | PHASE2 | COMPLETED | Hormone Replacement in Young Women With Premature Ovarian Failure |
| NCT00370019 | PHASE2 | WITHDRAWN | Effects of an Estrogen Replacement Therapy Skin Patch on Ovulation in Women With Premature Ovarian Failure |
| NCT00429494 | PHASE2 | COMPLETED | GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients |
| NCT03816852 | PHASE2 | SUSPENDED | The Safety and Efficiency Study of Mesenchymal Stem Cell (19#iSCLife®-POI) in Premature Ovarian Insufficiency |
| NCT04536467 | PHASE2 | UNKNOWN | Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients |
| NCT06117982 | PHASE2 | COMPLETED | The Impact of Granulocyte Colony Stimulating Factor on Premature Ovarian Insufficiency |
| NCT00040794 | PHASE2 | COMPLETED | Combination Chemotherapy, Radiation Therapy, and Gefitinib in Treating Patients With Stage III Non-Small Cell Lung Cancer |
| NCT00087412 | PHASE2 | COMPLETED | S0341: Erlotinib in Treating Patients With Advanced Primary Non-Small Cell Lung Cancer |
| NCT00118144 | PHASE2 | COMPLETED | Bortezomib in Treating Patients With Stage IIIB or Stage IV Lung Cancer |
| NCT00118183 | PHASE2 | 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 | PHASE2 | COMPLETED | Erlotinib Hydrochloride With or Without Carboplatin and Paclitaxel in Treating Patients With Stage III-IV Non-small Cell Lung Cancer |
| NCT00334815 | PHASE2 | 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 | PHASE2 | COMPLETED | S0536: Cetuximab, Paclitaxel, Carboplatin, and Bevacizumab in Treating Patients With Advanced Non-Small Cell Lung Cancer |
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): alopecia areata