Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPM2

Ligand: 2-APB (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
Published in: Br J Pharmacol

Ligand: ACAA (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid.
Published in: Br J Pharmacol

Ligand: ADP ribose (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): ADP-ribose gating of the calcium-permeable LTRPC2 channel revealed by Nudix motif homology.
Published in: Nature

Ligand: arachidonic acid (Metabolite)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): LTRPC2 Ca2+-permeable channel activated by changes in redox status confers susceptibility to cell death.
Published in: Mol Cell

Ligand: cADPR (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Cyclic ADP-ribose and hydrogen peroxide synergize with ADP-ribose in the activation of TRPM2 channels.
Published in: Mol Cell

Ligand: cADPR (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Nicotinic acid adenine dinucleotide phosphate and cyclic ADP-ribose regulate TRPM2 channels in T lymphocytes.
Published in: FASEB J

Ligand: cADPR (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion.
Published in: EMBO J

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  -
Reference (Journal): Inhibition of TRPM2 channels by the antifungal agents clotrimazole and econazole.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: econazole (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  -
Reference (Journal): Inhibition of TRPM2 channels by the antifungal agents clotrimazole and econazole.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: flufenamic acid (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  -
Reference (Journal): Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
Published in: Br J Pharmacol

Ligand: flufenamic acid (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  -
Reference (Journal): Flufenamic acid is a pH-dependent antagonist of TRPM2 channels.
Published in: Neuropharmacology

Ligand: GEA 3162 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Hydrogen peroxide and ADP-ribose induce TRPM2-mediated calcium influx and cation currents in microglia.
Published in: Am J Physiol, Cell Physiol

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Hydrogen-peroxide-induced toxicity of rat striatal neurones involves activation of a non-selective cation channel.
Published in: J Physiol (Lond.)

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): TRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase.
Published in: Br J Pharmacol

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Activation of the cation channel long transient receptor potential channel 2 (LTRPC2) by hydrogen peroxide. A splice variant reveals a mode of activation independent of ADP-ribose.
Published in: J Biol Chem

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): LTRPC2 Ca2+-permeable channel activated by changes in redox status confers susceptibility to cell death.
Published in: Mol Cell

Ligand: H+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: miconazole (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity:  -
Reference (Journal): Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
Published in: Br J Pharmacol

Ligand: NAADP (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 3.1 pEC50
Reference (Journal): Nicotinic acid adenine dinucleotide phosphate and cyclic ADP-ribose regulate TRPM2 channels in T lymphocytes.
Published in: FASEB J

Ligand: NAD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion.
Published in: EMBO J

Ligand: NAD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): LTRPC2 Ca2+-permeable channel activated by changes in redox status confers susceptibility to cell death.
Published in: Mol Cell

Ligand: NAD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Expression profile of the transient receptor potential (TRP) family in neutrophil granulocytes: evidence for currents through long TRP channel 2 induced by ADP-ribose and NAD.
Published in: Biochem J

Ligand: NAD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Immunocyte Ca2+ influx system mediated by LTRPC2.
Published in: Science

Ligand: OAADPR (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4 pKd
Reference (Journal): Metabolite of SIR2 reaction modulates TRPM2 ion channel.
Published in: J Biol Chem

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Pore collapse underlies irreversible inactivation of TRPM2 cation channel currents.
Published in: Proc Natl Acad Sci USA

Ligand: tatM2NX (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Characterization and Optimization of the Novel Transient Receptor Potential Melastatin 2 Antagonist tatM2NX.
Published in: Mol Pharmacol

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50