Target family: Platelet-activating factor receptor (type: gpcr)
Target: PAF receptor

Ligand: L659989 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor.
Published in: J Pharmacol Exp Ther

Ligand: 10-OBn-7α-F-gingkolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 10-OBn-epi-ginkgolide C (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 10-OBn-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 10-OBn-ginkgolide C (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 2-O-ethyl-PAF C-16 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
Published in: J Immunol Methods

Ligand: 2-O-methyl-PAF C-18 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
Published in: J Immunol Methods

Ligand: 7α-Cl-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-F-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-NHEt-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-NHMe-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-NH2-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-N3-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-OAc-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7α-OCOCH2Ph-ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: 7-epi-ginkgolide C (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: ABT-299 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Properties of ABT-299, a prodrug of A-85783, a highly potent platelet activating factor receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: ABT-491 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist.
Published in: Eur J Pharmacol

Ligand: apafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evidence for the presence of specific high affinity cytosolic binding sites for platelet-activating factor in human neutrophils.
Published in: Biochem Biophys Res Commun

Ligand: apafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis.
Published in: J Biol Chem

Ligand: bepafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacologic activity of bepafant (WEB 2170), a new and selective hetrazepinoic antagonist of platelet activating factor.
Published in: J Pharmacol Exp Ther

Ligand: bepafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological actions of PCA 4248, a new platelet-activating factor receptor antagonist: in vivo studies.
Published in: J Pharmacol Exp Ther

Ligand: BN 50739 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Evidence for the presence of specific high affinity cytosolic binding sites for platelet-activating factor in human neutrophils.
Published in: Biochem Biophys Res Commun

Ligand: CV-3988 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Inhibition by CV-3988 of the binding of [3H]-platelet activating factor (PAF) to the platelet.
Published in: Biochem Pharmacol

Ligand: CV-6209 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Novel phomactin analogues as PAF receptor ligands.
Published in: Bioorg Med Chem Lett

Ligand: CV-6209 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
Published in: J Biol Chem

Ligand: enantio PAF C-16 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5 pIC50
Reference (Journal): A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
Published in: J Immunol Methods

Ligand: foropafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pKi
Reference (Journal): Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes.
Published in: J Lipid Mediat

Ligand: ginkgolide A (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.
Published in: J Med Chem

Ligand: ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.
Published in: J Med Chem

Ligand: ginkgolide B (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Published in: J Med Chem

Ligand: ginkgolide C (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.
Published in: J Med Chem

Ligand: ginkgolide J (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.
Published in: J Med Chem

Ligand: israpafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
Published in: J Biol Chem

Ligand: methylcarbamyl PAF (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: PAF (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
Published in: J Biol Chem

Ligand: PAF (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
Published in: J Immunol Methods

Ligand: PAF (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis.
Published in: J Biol Chem

Ligand: PCA 4248 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pA2
Reference (Journal): Pharmacological actions of PCA 4248, a new platelet-activating factor receptor antagonist: in vivo studies.
Published in: J Pharmacol Exp Ther

Ligand: PCA 4248 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.44 pIC50
Reference (Journal): Pharmacological actions of PCA 4248, a new platelet-activating factor receptor antagonist: in vivo studies.
Published in: J Pharmacol Exp Ther

Ligand: RP-52770 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): [3H]52770 RP, a platelet-activating factor receptor antagonist, and tritiated platelet-activating factor label a common specific binding site in human polymorphonuclear leukocytes.
Published in: J Pharmacol Exp Ther

Ligand: rupatadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2007)
Primary target: no
Median affinity: 5.429999828338623 pKi
Reference (Journal): Designed multiple ligands. An emerging drug discovery paradigm.
Published in: J Med Chem

Ligand: SCH 37370 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): Conformational considerations in the design of dual antagonists of platelet-activating factor (PAF) and histamine.
Published in: Bioorg Med Chem

Ligand: SCH 40338 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): Conformational considerations in the design of dual antagonists of platelet-activating factor (PAF) and histamine.
Published in: Bioorg Med Chem

Ligand: SDZ 64-412 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Biological effects of the orally active platelet activating factor receptor antagonist SDZ 64-412.
Published in: J Pharmacol Exp Ther

Ligand: [3H]52770 RP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKd
Reference (Journal): [3H]52770 RP, a platelet-activating factor receptor antagonist, and tritiated platelet-activating factor label a common specific binding site in human polymorphonuclear leukocytes.
Published in: J Pharmacol Exp Ther

Ligand: [3H]apafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor.
Published in: J Immunol Methods

Ligand: [3H]apafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
Published in: J Biol Chem

Ligand: [3H]apafant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation.
Published in: J Biol Chem

Ligand: [3H]PAF (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular cloning and expression of platelet-activating factor receptor from human leukocytes.
Published in: J Biol Chem

Ligand: [3H]PAF (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation.
Published in: J Biol Chem