Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPV2

Ligand: 2-APB (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Activation properties of heterologously expressed mammalian TRPV2: evidence for species dependence.
Published in: J Biol Chem

Ligand: 2-APB (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
Published in: J Neurosci

Ligand: 2-APB (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): 2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3.
Published in: J Biol Chem

Ligand: 2-APB (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  -

Ligand: cannabidiol (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Median affinity: 4.5 pEC50
Reference (Journal): TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
Published in: J Neurosci

Ligand: cannabidiol (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Median affinity: 5.43 pEC50
Reference (Journal): TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
Published in: J Neurosci

Ligand: cannabinol (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.11 pEC50
Reference (Journal): TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
Published in: J Neurosci

Ligand: citral (Natural product)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Citral sensing by Transient [corrected] receptor potential channels in dorsal root ganglion neurons.
Published in: PLoS ONE

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 4.849999904632568 pEC50
Reference (Journal): TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
Published in: J Neurosci

Ligand: diphenylboronic anhydride (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol

Ligand: diphenylboronic anhydride (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Biphasic currents evoked by chemical or thermal activation of the heat-gated ion channel, TRPV3.
Published in: J Biol Chem

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Median affinity:  -
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol

Ligand: insulin-like growth factor 1 (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Translocation of a calcium-permeable cation channel induced by insulin-like growth factor-I.
Published in: Nat Cell Biol

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: loratadine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): Loratadine, an antihistaminic drug, suppresses the proliferation of endometrial stromal cells by inhibition of TRPV2.
Published in: Eur J Pharmacol

Ligand: lysophosphatidylcholine (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  -
Reference (Journal): Involvement of TRPV2 activation in intestinal movement through nitric oxide production in mice.
Published in: J Neurosci

Ligand: lysophosphatidylcholine (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  -
Reference (Journal): Lysophospholipids stimulate prostate cancer cell migration via TRPV2 channel activation.
Published in: Biochim Biophys Acta

Ligand: lysophosphatidylinositol (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  -
Reference (Journal): Lysophospholipids stimulate prostate cancer cell migration via TRPV2 channel activation.
Published in: Biochim Biophys Acta

Ligand: neuropeptide head activator (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The neuropeptide head activator induces activation and translocation of the growth-factor-regulated Ca(2+)-permeable channel GRC.
Published in: J Cell Sci

Ligand: probenecid (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1951)
Primary target: no
Median affinity: 4.5 pEC50
Reference (Journal): Transient receptor potential V2 expressed in sensory neurons is activated by probenecid.
Published in: Neurosci Lett

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): A capsaicin-receptor homologue with a high threshold for noxious heat.
Published in: Nature

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50

Ligand: SET2 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.340000152587891 pIC50
Reference (Journal): Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel.
Published in: J Med Chem

Ligand: SKF96365 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol

Ligand: tranilast (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity:  pIC50
Reference (Journal): Inhibition of proliferation of MCF-7 breast cancer cells by a blocker of Ca(2+)-permeable channel.
Published in: Cell Calcium

Ligand: TRIM (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Published in: Mol Pharmacol