Target family: Formylpeptide receptors (type: gpcr)
Target: FPR1

Ligand: WKYMVm (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pEC50
Reference (Journal): Utilization of two seven-transmembrane, G protein-coupled receptors, formyl peptide receptor-like 1 and formyl peptide receptor, by the synthetic hexapeptide WKYMVm for human phagocyte activation.
Published in: J Immunol

Ligand: WKYMVm (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: WKYMVm (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pEC50
Reference (Journal): The synthetic peptide Trp-Lys-Tyr-Met-Val-D-Met is a potent chemotactic agonist for mouse formyl peptide receptor.
Published in: J Immunol

Ligand: t-Boc-Met-Leu-Phe (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation.
Published in: J Immunol

Ligand: t-Boc-FLFLF (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E.
Published in: J Immunol

Ligand: t-Boc-FLFLF (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation.
Published in: J Immunol

Ligand: T20(DP178) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pEC50
Reference (Journal): The HIV-1 cell entry inhibitor T-20 potently chemoattracts neutrophils by specifically activating the N-formylpeptide receptor.
Published in: Biochem Biophys Res Commun

Ligand: T20(DP178) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pEC50
Reference (Journal): T20/DP178, an ectodomain peptide of human immunodeficiency virus type 1 gp41, is an activator of human phagocyte N-formyl peptide receptor.
Published in: Blood

Ligand: [3H]fMet-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): The oligopeptide chemotactic factor receptor on human polymorphonuclear leukocyte membranes exists in two affinity states.
Published in: Biochem Biophys Res Commun

Ligand: [125I]CHIPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKd
Reference (Journal): N-terminal residues of the chemotaxis inhibitory protein of Staphylococcus aureus are essential for blocking formylated peptide receptor but not C5a receptor.
Published in: J Immunol

Ligand: [125I]cathepsin G (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKd
Reference (Journal): Identification of neutrophil granule protein cathepsin G as a novel chemotactic agonist for the G protein-coupled formyl peptide receptor.
Published in: J Immunology

Ligand: sufinpyrazone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 5 pIC50
Reference (Journal): High-throughput screening with HyperCyt flow cytometry to detect small molecule formylpeptide receptor ligands.
Published in: J Biomol Screen

Ligand: spinorphin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.3 pIC50
Reference (Journal): A structural homologue of the N-formyl peptide receptor. Characterization and chromosome mapping of a peptide chemoattractant receptor family.
Published in: J Biol Chem

Ligand: spinorphin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 3.9 pEC50
Reference (Journal): The endogenous opioid spinorphin blocks fMet-Leu-Phe-induced neutrophil chemotaxis by acting as a specific antagonist at the N-formylpeptide receptor subtype FPR.
Published in: J Immunol

Ligand: spinorphin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.3 pIC50
Reference (Journal): The endogenous opioid spinorphin blocks fMet-Leu-Phe-induced neutrophil chemotaxis by acting as a specific antagonist at the N-formylpeptide receptor subtype FPR.
Published in: J Immunol

Ligand: pyrazolone, 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: Met-Met-Trp-Leu-Leu (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pEC50
Reference (Journal): Tethered ligand library for discovery of peptide agonists.
Published in: J Biol Chem

Ligand: 3570-0208 [PMID:19807662] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Discovery of selective probes and antagonists for G-protein-coupled receptors FPR/FPRL1 and GPR30.
Published in: Curr Top Med Chem

Ligand: AG-09/1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Identification of novel small-molecule agonists for human formyl peptide receptors and pharmacophore models of their recognition.
Published in: Mol Pharmacol

Ligand: AG-11/03 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Molecular docking of 2-(benzimidazol-2-ylthio)-N-phenylacetamide-derived small-molecule agonists of human formyl peptide receptor 1.
Published in: J Mol Model

Ligand: AG-14 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pEC50
Reference (Journal): High-throughput screening for small-molecule activators of neutrophils: identification of novel N-formyl peptide receptor agonists.
Published in: Mol Pharmacol

Ligand: annexin I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pEC50
Reference (Journal): Impaired T cell activation and increased Th2 lineage commitment in Annexin-1-deficient T cells.
Published in: Eur J Immunol

Ligand: annexin I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pEC50
Reference (Journal): Involvement of the receptor for formylated peptides in the in vivo anti-migratory actions of annexin 1 and its mimetics.
Published in: Am J Pathol

Ligand: annexin I-(2-26) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Leukocyte antiadhesive actions of annexin 1: ALXR- and FPR-related anti-inflammatory mechanisms.
Published in: Blood

Ligand: annexin I-(2-26) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A novel ligand of the formyl peptide receptor: annexin I regulates neutrophil extravasation by interacting with the FPR.
Published in: Mol Cell

Ligand: BMS-986235 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
Published in: J Med Chem

Ligand: BMS-986235 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
Published in: J Med Chem

Ligand: BVT173187 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): A non-peptide receptor inhibitor with selectivity for one of the neutrophil formyl peptide receptors, FPR 1.
Published in: Biochem Pharmacol

Ligand: chenodeoxycholic acid (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1983), EMA (2017)
Median affinity: 4 pKi
Reference (Journal): Characterization of chenodeoxycholic acid as an endogenous antagonist of the G-coupled formyl peptide receptors.
Published in: Inflamm Res

Ligand: compound R-(-)-5f [PMID: 22607879] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Synthesis, enantioresolution, and activity profile of chiral 6-methyl-2,4-disubstituted pyridazin-3(2H)-ones as potent N-formyl peptide receptor agonists.
Published in: Bioorg Med Chem

Ligand: cyclosporin A (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and UK (1983), EMA (2015)
Median affinity:  pEC50
Reference (Journal): Inhibitory effects of spinorphin, a novel endogenous regulator, on chemotaxis, O2- generation, and exocytosis by N-formylmethionyl-leucyl-phenylalanine (FMLP)-stimulated neutrophils.
Published in: Biochem Pharmacol

Ligand: cyclosporin H (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E.
Published in: J Immunol

Ligand: cyclosporin H (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The immunosuppressant cyclosporin A antagonizes human formyl peptide receptor through inhibition of cognate ligand binding.
Published in: J Immunol

Ligand: deoxycholic acid (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2015)
Median affinity: 4 pKi
Reference (Journal): Regulatory effects of deoxycholic acid, a component of the anti-inflammatory traditional Chinese medicine Niuhuang, on human leukocyte response to chemoattractants.
Published in: Biochem Pharmacol

Ligand: diamide 7 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Discovery of small molecule human FPR1 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: fMet-Ile-Phe-Leu (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: fMet-Ile-Phe-Leu (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.5 pEC50
Reference (Journal): A series of six ligands for the human formyl peptide receptor: tetrapeptides with high chemotactic potency and efficacy.
Published in: Proc Natl Acad Sci USA

Ligand: fMet-Ile-Val-Ile-Leu (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pEC50
Reference (Journal): Human mitochondria-derived N-formylated peptides are novel agonists equally active on FPR and FPRL1, while Listeria monocytogenes-derived peptides preferentially activate FPR.
Published in: Eur J Immunol

Ligand: fMet-Ile-Val-Thr-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pEC50
Reference (Journal): Human mitochondria-derived N-formylated peptides are novel agonists equally active on FPR and FPRL1, while Listeria monocytogenes-derived peptides preferentially activate FPR.
Published in: Eur J Immunol

Ligand: fMet-Ile-Val-Thr-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.7 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: fMet-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pEC50
Reference (Journal): N-formylpeptides induce two distinct concentration optima for mouse neutrophil chemotaxis by differential interaction with two N-formylpeptide receptor (FPR) subtypes. Molecular characterization of FPR2, a second mouse neutrophil FPR.
Published in: J Exp Med

Ligand: fMet-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Further studies on the structural requirements for synthetic peptide chemoattractants.
Published in: Biochemistry

Ligand: fMet-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The structure-activity relations of synthetic peptides as chemotactic factors and inducers of lysosomal secretion for neutrophils.
Published in: J Exp Med

Ligand: fMet-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pEC50
Reference (Journal): Identification of formyl peptides from Listeria monocytogenes and Staphylococcus aureus as potent chemoattractants for mouse neutrophils.
Published in: J Immunol

Ligand: fMet-Leu-Phe-Glu (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol