Target family: Complement peptide receptors (type: gpcr)
Target: C5a<sub>1</sub> receptor

Ligand: DF2593A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief.
Published in: Proc Natl Acad Sci USA

Ligand: DF3016A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Correction to: The Novel C5aR Antagonist DF3016A Protects Neurons Against Ischemic Neuroinflammatory Injury.
Published in: Neurotox Res

Ligand: Eu-DTPA-[Ser27, Nle70]hC5a (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Development of Synthetic Human and Mouse C5a: Application to Binding and Functional Assays <i>In Vitro</i> and <i>In Vivo</i>.
Published in: ACS Pharmacol Transl Sci

Ligand: N-methyl-Phe-Lys-Pro-D-Cha-Cha-D-Arg-CO2H (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Development of C5a receptor antagonists. Differential loss of functional responses.
Published in: J Immunol

Ligand: N-methyl-Phe-Lys-Pro-D-Cha-Cha-D-Arg-CO2H (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Structure-function studies in a series of carboxyl-terminal octapeptide analogues of anaphylatoxin C5a.
Published in: J Med Chem

Ligand: N-methyl-Phe-Lys-Pro-D-Cha-Trp-D-Arg-CO2H (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Development of C5a receptor antagonists. Differential loss of functional responses.
Published in: J Immunol

Ligand: JPE1375 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.
Published in: Bioorg Med Chem Lett

Ligand: L-156,602 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Anti-inflammatory effects and specificity of L-156,602: comparison of effects on concanavalin A and zymosan-induced footpad edema, and contact sensitivity response.
Published in: Immunopharmacology

Ligand: lactomedin 1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Partial ligand-receptor engagement yields functional bias at the human complement receptor, C5aR1.
Published in: J Biol Chem

Ligand: lactomedin 1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Bioactive peptides derived from natural proteins with respect to diversity of their receptors and physiological effects.
Published in: Peptides

Ligand: NDT9513727 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.940000057220459 pIC50
Reference (Journal): Identification and characterization of NDT 9513727 [N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine], a novel, orally bioavailable C5a receptor inverse agonist.
Published in: J Pharmacol Exp Ther

Ligand: NDT9520492 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular characterization of the gerbil C5a receptor and identification of a transmembrane domain V amino acid that is crucial for small molecule antagonist interaction.
Published in: J Biol Chem

Ligand: PMX205 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function.
Published in: Biochem Pharmacol

Ligand: PMX205 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.
Published in: Mol Pharmacol

Ligand: PMX53 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.
Published in: Mol Pharmacol

Ligand: PMX53 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes.
Published in: Inflammation

Ligand: PMX53 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Differential effects of complement activation products c3a and c5a on cardiovascular function in hypertensive pregnant rats.
Published in: J Pharmacol Exp Ther

Ligand: PMX53 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Insights into the mechanism of C5aR inhibition by PMX53 via implicit solvent molecular dynamics simulations and docking.
Published in: BMC Biophys

Ligand: ribosomal protein S19 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular mechanism of monocyte predominant infiltration in chronic inflammation: mediation by a novel monocyte chemotactic factor, S19 ribosomal protein dimer.
Published in: Pathol Int

Ligand: RPR121154 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pIC50
Reference (Journal): New non-peptide C5a receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: [125I]C5a (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): Characterization of a C5a receptor on human polymorphonuclear leukocytes (PMN).
Published in: J Immunol

Ligand: W54011 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Identification of a potent and orally active non-peptide C5a receptor antagonist.
Published in: J Biol Chem

Ligand: YSFKPMPLaR (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Biologically active conformer of the effector region of human C5a and modulatory effects of N-terminal receptor binding determinants on activity.
Published in: J Med Chem

Ligand: YSFKPMPLaR (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes.
Published in: Inflammation