Target family: Formylpeptide receptors (type: gpcr)
Target: FPR2

Ligand: SHAAGtide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.72 pEC50
Reference (Journal): Proinflammatory proteases liberate a discrete high-affinity functional FPRL1 (CCR12) ligand from CCL23.
Published in: J Immunol

Ligand: SHAAGtide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.72 pEC50
Reference (Journal): A truncated form of CKbeta8-1 is a potent agonist for human formyl peptide-receptor-like 1 receptor.
Published in: Br J Pharmacol

Ligand: serum amyloid A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pEC50
Reference (Journal): A seven-transmembrane, G protein-coupled receptor, FPRL1, mediates the chemotactic activity of serum amyloid A for human phagocytic cells.
Published in: J Exp Med

Ligand: sCKβ8-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A truncated form of CKbeta8-1 is a potent agonist for human formyl peptide-receptor-like 1 receptor.
Published in: Br J Pharmacol

Ligand: RvD1-ME (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11.430000305175781 pEC50
Reference (Journal): Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs.
Published in: Am J Pathol

Ligand: resolvin D1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 11.9 pEC50
Reference (Journal): Resolvin D1 binds human phagocytes with evidence for proresolving receptors.
Published in: Proc Natl Acad Sci USA

Ligand: quin-C7 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.18 pEC50
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1.
Published in: Mol Pharmacol

Ligand: quin-C1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.72 pEC50
Reference (Journal): A novel nonpeptide ligand for formyl peptide receptor-like 1.
Published in: Mol Pharmacol

Ligand: quin-C1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: pyrazolone, 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.92 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: pyrazolone, 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pEC50
Reference (Journal): Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
Published in: Bioorg Med Chem Lett

Ligand: PSMα3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.67 pEC50
Reference (Journal): Human formyl peptide receptor 2 senses highly pathogenic Staphylococcus aureus.
Published in: Cell Host Microbe

Ligand: PrP106-126 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): Distinct signaling cascades elicited by different formyl Peptide receptor 2 (FPR2) agonists.
Published in: Int J Mol Sci

Ligand: PBP10 (Peptide)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7 pIC50
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: N36 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): N36, a synthetic N-terminal heptad repeat domain of the HIV-1 envelope protein gp41, is an activator of human phagocytes.
Published in: Clin Immunol

Ligand: MMK-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pEC50
Reference (Journal): Identification of surrogate agonists for the human FPRL-1 receptor by autocrine selection in yeast.
Published in: Nat Biotechnol

Ligand: MMK-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pEC50
Reference (Journal): Synthetic peptide MMK-1 is a highly specific chemotactic agonist for leukocyte FPRL1.
Published in: J Leukoc Biol

Ligand: MHC binding peptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pIC50
Reference (Journal): Activation of lipoxin A(4) receptors by aspirin-triggered lipoxins and select peptides evokes ligand-specific responses in inflammation.
Published in: J Exp Med

Ligand: LXA4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Identification of a human cDNA encoding a functional high affinity lipoxin A4 receptor.
Published in: J Exp Med

Ligand: LXA4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Lipoxin recognition sites. Specific binding of labeled lipoxin A4 with human neutrophils.
Published in: J Biol Chem

Ligand: LXA4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 12 pEC50
Reference (Journal): Resolvin D1 binds human phagocytes with evidence for proresolving receptors.
Published in: Proc Natl Acad Sci USA

Ligand: LL-37 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): LL-37, the neutrophil granule- and epithelial cell-derived cathelicidin, utilizes formyl peptide receptor-like 1 (FPRL1) as a receptor to chemoattract human peripheral blood neutrophils, monocytes, and T cells.
Published in: J Exp Med

Ligand: isopropylureido-FLFLF (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Selective inhibition of N-formylpeptide-induced neutrophil activation by carbamate-modified peptide analogues.
Published in: Biochemistry

Ligand: humanin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Humanin, a newly identified neuroprotective factor, uses the G protein-coupled formylpeptide receptor-like-1 as a functional receptor.
Published in: J Immunol

Ligand: humanin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.46 pEC50
Reference (Journal): N-Formylated humanin activates both formyl peptide receptor-like 1 and 2.
Published in: Biochem Biophys Res Commun

Ligand: Hp(2-20) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): A proinflammatory peptide from Helicobacter pylori activates monocytes to induce lymphocyte dysfunction and apoptosis.
Published in: J Clin Invest

Ligand: FPRL1-inhibitor protein (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): A new staphylococcal anti-inflammatory protein that antagonizes the formyl peptide receptor-like 1.
Published in: J Immunol

Ligand: F peptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): A synthetic peptide derived from human immunodeficiency virus type 1 gp120 downregulates the expression and function of chemokine receptors CCR5 and CXCR4 in monocytes by activating the 7-transmembrane G-protein-coupled receptor FPRL1/LXA4R.
Published in: Blood

Ligand: fMet-Met-Tyr-Ala-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.32 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: fMet-Met-Tyr-Ala-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.82 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-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.37 pKd
Reference (Journal): Multiple domains of the N-formyl peptide receptor are required for high-affinity ligand binding. Construction and analysis of chimeric N-formyl peptide receptors.
Published in: J Biol Chem

Ligand: fMet-Ile-Val-Thr-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 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: 5.55 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-Ile-Val-Thr-Leu-Phe (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.55 pEC50
Reference (Journal): Functional characterization of three mouse formyl peptide receptors.
Published in: Mol Pharmacol

Ligand: F2L (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): F2L, a peptide derived from heme-binding protein, chemoattracts mouse neutrophils by specifically activating Fpr2, the low-affinity N-formylpeptide receptor.
Published in: J Immunol

Ligand: CRAMP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Mouse cathelin-related antimicrobial peptide chemoattracts leukocytes using formyl peptide receptor-like 1/mouse formyl peptide receptor-like 2 as the receptor and acts as an immune adjuvant.
Published in: J Immunol

Ligand: compound R-(-)-5f [PMID: 22607879] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.269999980926514 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: compound 1754-31 [PMID: 23788657] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.09 pIC50
Reference (Journal): Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.
Published in: Mol Pharmacol

Ligand: CGEN-855A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.72 pIC50
Reference (Journal): A novel peptide agonist of formyl-peptide receptor-like 1 (ALX) displays anti-inflammatory and cardioprotective effects.
Published in: J Pharmacol Exp Ther

Ligand: CGEN-855A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.27 pKi
Reference (Journal): A novel peptide agonist of formyl-peptide receptor-like 1 (ALX) displays anti-inflammatory and cardioprotective effects.
Published in: J Pharmacol Exp Ther

Ligand: BMS-986235 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 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: 8.300000190734863 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: ATLa2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Novel 3-oxa lipoxin A4 analogues with enhanced chemical and metabolic stability have anti-inflammatory activity in vivo.
Published in: J Med Chem

Ligand: aspirin-triggered resolvin D1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11.100000381469727 pEC50
Reference (Journal): Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs.
Published in: Am J Pathol

Ligand: aspirin triggered lipoxin A4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

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: 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): Annexin 1 and its bioactive peptide inhibit neutrophil-endothelium interactions under flow: indication of distinct receptor involvement.
Published in: Blood

Ligand: annexin I-(2-26) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Endogenous lipid- and peptide-derived anti-inflammatory pathways generated with glucocorticoid and aspirin treatment activate the lipoxin A4 receptor.
Published in: Nat Med

Ligand: annexin I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKd
Reference (Journal): Endogenous lipid- and peptide-derived anti-inflammatory pathways generated with glucocorticoid and aspirin treatment activate the lipoxin A4 receptor.
Published in: Nat Med

Ligand: amyloid β (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): Amyloid (beta)42 activates a G-protein-coupled chemoattractant receptor, FPR-like-1.
Published in: J Neurosci

Ligand: amyloid β (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): Amyloid-beta induces chemotaxis and oxidant stress by acting at formylpeptide receptor 2, a G protein-coupled receptor expressed in phagocytes and brain.
Published in: J Biol Chem

Ligand: AG-26 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 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: ACT-389949 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pEC50
Reference (Journal): Biomarker-guided clinical development of the first-in-class anti-inflammatory FPR2/ALX agonist ACT-389949.
Published in: Br J Clin Pharmacol

Ligand: 1R-11 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Asymmetric synthesis and biological evaluation of imidazole- and oxazole-containing synthetic lipoxin A<sub>4</sub> mimetics (sLXms).
Published in: Eur J Med Chem