Target family: P2X receptors (type: lgic)
Target: P2X7

Ligand: AZ11657312 (salt free) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 6.099999904632568 pA2
Reference (Webpage): AZ11657312.

Ligand: brilliant blue G (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Brilliant blue G selectively blocks ATP-gated rat P2X(7) receptors.
Published in: Mol Pharmacol

Ligand: BzATP (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4 pEC50
Reference (Journal): Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
Published in: Br J Pharmacol

Ligand: BzATP (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
Published in: Br J Pharmacol

Ligand: BzATP (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.329999923706055 pEC50
Reference (Journal): Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
Published in: Br J Pharmacol

Ligand: chelerythrine (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 5.25 pIC50
Reference (Journal): Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor.
Published in: Br J Pharmacol

Ligand: clemastine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity:  -
Reference (Journal): Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
Published in: J Biol Chem

Ligand: compound 16i [PMID: 31525963] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.639999866485596 pIC50
Reference (Journal): Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
Published in: J Med Chem

Ligand: decavanadate (Inorganic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pA2
Reference (Journal): Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors.
Published in: Eur J Pharmacol

Ligand: GSK1370319A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.320000171661377 pIC50
Reference (Journal): Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
Published in: J Med Chem

Ligand: GSK1482160 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
Published in: J Med Chem

Ligand: GSK1482160 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Published in: Bioorg Med Chem Lett

Ligand: GSK1482160 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Published in: Bioorg Med Chem Lett

Ligand: GSK1482160 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.9399995803833 pKd
Reference (Journal): Characterization of <sup>11</sup>C-GSK1482160 for Targeting the P2X7 Receptor as a Biomarker for Neuroinflammation.
Published in: J Nucl Med

Ligand: GW791343 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Negative and positive allosteric modulators of the P2X(7) receptor.
Published in: Br J Pharmacol

Ligand: GW791343 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Negative and positive allosteric modulators of the P2X(7) receptor.
Published in: Br J Pharmacol

Ligand: GW791343 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
Published in: Br J Pharmacol

Ligand: GW791343 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
Published in: Br J Pharmacol

Ligand: ITH15004 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.050000190734863 pIC50
Reference (Journal): Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
Published in: J Med Chem

Ligand: ivermectin (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1996), UK (2015)
Primary target: no
Median affinity:  -
Reference (Journal): Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.
Published in: Br J Pharmacol

Ligand: JNJ-47965567 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.
Published in: Br J Pharmacol

Ligand: JNJ-47965567 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.
Published in: Br J Pharmacol

Ligand: KN62 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes.
Published in: Br J Pharmacol

Ligand: KN62 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor.
Published in: Br J Pharmacol

Ligand: LL-37 (Peptide)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The human cathelicidin LL-37 modulates the activities of the P2X7 receptor in a structure-dependent manner.
Published in: J Biol Chem

Ligand: oxidised ATP (Synthetic organic)
Interaction type: Antagonist
Action: Irreversible inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Oxidized ATP. An irreversible inhibitor of the macrophage purinergic P2Z receptor.
Published in: J Biol Chem

Ligand: PF-04905428 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Patent): Benzamide inhibitors of the P2X7 receptor

Ligand: PF-04905428 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Published in: Bioorg Med Chem Lett

Ligand: polymyxin B (Peptide)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1964, no prior history available)
Primary target: no
Median affinity:  -
Reference (Journal): The antibiotic polymyxin B modulates P2X7 receptor function.
Published in: J Immunol