Target family: P2X receptors (type: lgic)
Target: P2X4

Ligand: PSB-12062 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): P2X receptors as drug targets.
Published in: Mol Pharmacol

Ligand: PSB-12062 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Medicinal chemistry of adenosine, P2Y and P2X receptors.
Published in: Neuropharmacology

Ligand: PSB-12054 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.
Published in: J Med Chem

Ligand: PPADS (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: PPADS (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: paroxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: no
Median affinity:  pIC50
Reference (Journal): P2X receptors as drug targets.
Published in: Mol Pharmacol

Ligand: paroxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Medicinal chemistry of adenosine, P2Y and P2X receptors.
Published in: Neuropharmacology

Ligand: NP-1815-PX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): A novel P2X4 receptor-selective antagonist produces anti-allodynic effect in a mouse model of herpetic pain.
Published in: Sci Rep

Ligand: nimodipine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1988)
Primary target: no
Median affinity:  -
Reference (Journal): Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor.
Published in: Molecules

Ligand: ivermectin (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1996), UK (2015)
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): Allosteric control of gating and kinetics at P2X(4) receptor channels.
Published in: J Neurosci

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

Ligand: BX-430 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Medicinal chemistry of adenosine, P2Y and P2X receptors.
Published in: Neuropharmacology

Ligand: BX-430 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): P2X receptors as drug targets.
Published in: Mol Pharmacol

Ligand: BAY-1797 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Discovery and Characterization of the Potent and Selective P2X4 Inhibitor <i>N</i>-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile.
Published in: J Med Chem

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pEC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pEC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Purine and pyrimidine (P2) receptors as drug targets.
Published in: J Med Chem

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Purine and pyrimidine (P2) receptors as drug targets.
Published in: J Med Chem

Ligand: amlodipine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Approval source: FDA (1992), EMA (2007)
Primary target: no
Median affinity:  -
Reference (Journal): Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor.
Published in: Molecules

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

Ligand: αβ-meATP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pEC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: αβ-meATP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pEC50
Reference (Journal): Functional characterization of the P2X(4) receptor orthologues.
Published in: Br J Pharmacol

Ligand: 5-BDBD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): P2X receptors as drug targets.
Published in: Mol Pharmacol

Ligand: 5-BDBD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Medicinal chemistry of adenosine, P2Y and P2X receptors.
Published in: Neuropharmacology