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

Ligand: A8Δ71-73 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.57 pIC50
Reference (Journal): C5a mutants are potent antagonists of the C5a receptor (CD88) and of C5L2: position 69 is the locus that determines agonism or antagonism.
Published in: J Biol Chem

Ligand: AcPhe-Orn-Pro-D-Cha-Trp-Arg (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pIC50
Reference (Journal): Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a.
Published in: J Med Chem

Ligand: ACT-1014-6470 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Effect of Severe Renal Impairment on Pharmacokinetics, Safety, and Tolerability of ACT-1014-6470, a Novel Oral Complement Factor 5a Receptor 1 Antagonist.
Published in: Clin Pharmacol Drug Dev

Ligand: avacopan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study.
Published in: PLoS ONE

Ligand: BM213 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.230000019073486 pEC50
Reference (Journal): Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity.
Published in: J Med Chem

Ligand: BM221 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pEC50
Reference (Journal): Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity.
Published in: J Med Chem

Ligand: C089 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Development of C5a receptor antagonists. Differential loss of functional responses.
Published in: J Immunol

Ligand: C5a (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): S19 ribosomal protein cross-linked dimer causes monocyte-predominant infiltration by means of molecular mimicry to complement C5a.
Published in: Lab Invest

Ligand: C5a (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of antagonists of the C5a receptor.
Published in: Br J Pharmacol

Ligand: C5a (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of antagonists of the C5a receptor.
Published in: Br J Pharmacol

Ligand: C5a (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Comparative agonist/antagonist responses in mutant human C5a receptors define the ligand binding site.
Published in: J Biol Chem

Ligand: C5a des-Arg (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The orphan receptor C5L2 has high affinity binding sites for complement fragments C5a and C5a des-Arg(74).
Published in: J Biol Chem