Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPA1

Ligand: 1,6-hexamethylene diisocyanate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases.
Published in: FASEB J

Ligand: 1'-acetoxychavicol acetate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.8 pEC50
Reference (Journal): Galangal pungent component, 1'-acetoxychavicol acetate, activates TRPA1.
Published in: Biosci Biotechnol Biochem

Ligand: 2-iodoacetamide (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 3.45 pEC50
Reference (Journal): Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
Published in: Nature

Ligand: 2-pentenal (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Published in: J Med Chem

Ligand: 4-hydroxynonenal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): 4-Hydroxynonenal, an endogenous aldehyde, causes pain and neurogenic inflammation through activation of the irritant receptor TRPA1.
Published in: Proc Natl Acad Sci USA

Ligand: 4-hydroxynonenal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): An ion channel essential for sensing chemical damage.
Published in: J Neurosci

Ligand: 4-oxo-nonenal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.7 pEC50
Reference (Journal): Transient receptor potential A1 is a sensory receptor for multiple products of oxidative stress.
Published in: J Neurosci

Ligand: A-967079 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.
Published in: Pain

Ligand: acetaldehyde (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 2.9 pEC50
Reference (Journal): Transient receptor potential A1 mediates acetaldehyde-evoked pain sensation.
Published in: Eur J Neurosci

Ligand: acetaldehyde (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.1 pEC50
Reference (Journal): Transient receptor potential A1 mediates acetaldehyde-evoked pain sensation.
Published in: Eur J Neurosci

Ligand: acrolein (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents.
Published in: Cell

Ligand: allicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.9 pEC50
Reference (Journal): The pungency of garlic: activation of TRPA1 and TRPV1 in response to allicin.
Published in: Curr Biol

Ligand: allicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): Pungent products from garlic activate the sensory ion channel TRPA1.
Published in: Proc Natl Acad Sci USA

Ligand: allyl isothiocyanate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.7 pEC50
Reference (Journal): Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin.
Published in: Neuron

Ligand: allyl isothiocyanate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1.
Published in: Nature

Ligand: allyl isothiocyanate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pEC50
Reference (Journal): TRP channel activation by reversible covalent modification.
Published in: Proc Natl Acad Sci USA

Ligand: AM-0902 (Synthetic organic)
Interaction type: Inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Published in: J Med Chem

Ligand: AM-0902 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Published in: J Med Chem

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 3.3 pIC50
Reference (Journal): Nociceptor and hair cell transducer properties of TRPA1, a channel for pain and hearing.
Published in: J Neurosci

Ligand: AP18 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.35 pIC50
Reference (Journal): A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition.
Published in: Mol Pain

Ligand: AP18 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.51 pIC50
Reference (Journal): A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition.
Published in: Mol Pain

Ligand: AP18 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition.
Published in: Mol Pain

Ligand: apomorphine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity: 5.1 pEC50
Reference (Journal): Apomorphine is a bimodal modulator of TRPA1 channels.
Published in: Mol Pharmacol

Ligand: artepillin C (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.74 pEC50
Reference (Journal): Artepillin C, a major ingredient of Brazilian propolis, induces a pungent taste by activating TRPA1 channels.
Published in: PLoS ONE

Ligand: ASP7663 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.269999980926514 pEC50
Reference (Journal): Effects of novel TRPA1 receptor agonist ASP7663 in models of drug-induced constipation and visceral pain.
Published in: Eur J Pharmacol

Ligand: ASP7663 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pEC50
Reference (Journal): Effects of novel TRPA1 receptor agonist ASP7663 in models of drug-induced constipation and visceral pain.
Published in: Eur J Pharmacol

Ligand: ASP7663 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Effects of novel TRPA1 receptor agonist ASP7663 in models of drug-induced constipation and visceral pain.
Published in: Eur J Pharmacol

Ligand: auranofin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1985)
Median affinity: 6 pEC50
Reference (Journal): Stimulation of human TRPA1 channels by clinical concentrations of the antirheumatic drug auranofin.
Published in: Am J Physiol, Cell Physiol

Ligand: benzoquinone (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): TRPA1 mediates spinal antinociception induced by acetaminophen and the cannabinoid Δ(9)-tetrahydrocannabiorcol.
Published in: Nat Commun

Ligand: benzyl bromide (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.9 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases.
Published in: FASEB J

Ligand: bromoacetone (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases.
Published in: FASEB J

Ligand: camphor (Natural product)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 4.2 pIC50
Reference (Journal): More than cool: promiscuous relationships of menthol and other sensory compounds.
Published in: Mol Cell Neurosci

Ligand: cannabichromene (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Published in: J Med Chem

Ligand: cannabidiol (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Primary target: no
Median affinity: 6.320000171661377 pEC50
Reference (Journal): Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, <i>Cannabis sativa</i> L., Is a Selective Thermo-TRP Modulator.
Published in: J Nat Prod

Ligand: cannabidiolic acid (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.920000076293945 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Published in: J Med Chem

Ligand: cannabigerol (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pEC50
Reference (Journal): Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV.
Published in: J Nat Prod

Ligand: cannabigeroquinone (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.110000133514404 pEC50
Reference (Journal): Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV.
Published in: J Nat Prod

Ligand: Cd2+ (Inorganic)
Interaction type: Activator
Action: Activation
Median affinity: 5.85 pEC50
Reference (Journal): Clioquinol and pyrithione activate TRPA1 by increasing intracellular Zn2+.
Published in: Proc Natl Acad Sci USA

Ligand: Cd2+ (Inorganic)
Interaction type: Activator
Action: Activation
Median affinity: 5.68 pEC50
Reference (Journal): Clioquinol and pyrithione activate TRPA1 by increasing intracellular Zn2+.
Published in: Proc Natl Acad Sci USA

Ligand: Cd2+ (Inorganic)
Interaction type: Activator
Action: Activation
Median affinity: 5.68 pEC50
Reference (Journal): Involvement of TRPA1 activation in acute pain induced by cadmium in mice.
Published in: Mol Pain

Ligand: Cd2+ (Inorganic)
Interaction type: Activator
Action: Activation
Median affinity: 5.85 pEC50
Reference (Journal): Involvement of TRPA1 activation in acute pain induced by cadmium in mice.
Published in: Mol Pain

Ligand: chlorobenzylidene malononitrile (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor.
Published in: Toxicol Appl Pharmacol

Ligand: chloropicrin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases.
Published in: FASEB J

Ligand: cinnamaldehyde (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pEC50
Reference (Journal): Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin.
Published in: Neuron

Ligand: crotylaldehyde (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): Cigarette smoke-induced neurogenic inflammation is mediated by alpha,beta-unsaturated aldehydes and the TRPA1 receptor in rodents.
Published in: J Clin Invest

Ligand: Cu2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.22 pEC50
Reference (Journal): Involvement of TRPA1 activation in acute pain induced by cadmium in mice.
Published in: Mol Pain

Ligand: Cu2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.89 pEC50
Reference (Journal): Involvement of TRPA1 activation in acute pain induced by cadmium in mice.
Published in: Mol Pain

Ligand: Cu2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.89 pEC50
Reference (Journal): Clioquinol and pyrithione activate TRPA1 by increasing intracellular Zn2+.
Published in: Proc Natl Acad Sci USA

Ligand: Cu2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.22 pEC50
Reference (Journal): Clioquinol and pyrithione activate TRPA1 by increasing intracellular Zn2+.
Published in: Proc Natl Acad Sci USA

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1.
Published in: Nature

Ligand: dibenzoxazepine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 7.2 pEC50
Reference (Journal): Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor.
Published in: Toxicol Appl Pharmacol

Ligand: dibutyl phthalate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): TRPA1 and TRPV1 activation is a novel adjuvant effect mechanism in contact hypersensitivity.
Published in: J Neuroimmunol

Ligand: docosahexaenoic acid (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.4 pEC50
Reference (Journal): TRPA1 is a polyunsaturated fatty acid sensor in mammals.
Published in: PLoS ONE

Ligand: eugenol (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin.
Published in: Neuron

Ligand: flufenamic acid (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Median affinity: 3.8 pEC50
Reference (Journal): Activation of TRPA1 channels by fenamate nonsteroidal anti-inflammatory drugs.
Published in: Pflugers Arch

Ligand: formalin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 3.4000000953674316 pEC50
Reference (Journal): TRPA1 mediates formalin-induced pain.
Published in: Proc Natl Acad Sci USA

Ligand: formalin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 3.4000000953674316 pEC50
Reference (Journal): An ion channel essential for sensing chemical damage.
Published in: J Neurosci

Ligand: GDC-0334 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment.
Published in: J Exp Med

Ligand: GDC-6599 (Synthetic organic)
Interaction type: Antagonist
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.029999732971191 pIC50
Reference (Patent): Oxadiazole transient receptor potential channel inhibitors

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Nociceptor and hair cell transducer properties of TRPA1, a channel for pain and hearing.
Published in: J Neurosci

Ligand: gentamicin (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1970)
Median affinity: 5.2 pIC50
Reference (Journal): Nociceptor and hair cell transducer properties of TRPA1, a channel for pain and hearing.
Published in: J Neurosci

Ligand: gingerol (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin.
Published in: Neuron

Ligand: HC030031 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.2 pIC50
Reference (Journal): TRPA1 mediates formalin-induced pain.
Published in: Proc Natl Acad Sci USA

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 3.6 pEC50
Reference (Journal): Activation of transient receptor potential ankyrin 1 by hydrogen peroxide.
Published in: Eur J Neurosci

Ligand: H2O2 (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 3.6 pEC50
Reference (Journal): Transient receptor potential A1 is a sensory receptor for multiple products of oxidative stress.
Published in: J Neurosci

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures.
Published in: Cell

Ligand: isoflurane (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1979)
Median affinity: 3.7 pEC50
Reference (Journal): General anesthetics activate a nociceptive ion channel to enhance pain and inflammation.
Published in: Proc Natl Acad Sci USA

Ligand: isopentenyl diphosphate (Metabolite)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.1 pIC50
Reference (Journal): Resolvin D1 attenuates activation of sensory transient receptor potential channels leading to multiple anti-nociception.
Published in: Br J Pharmacol

Ligand: isovelleral (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.3 pEC50
Reference (Journal): TRPA1 mediates the noxious effects of natural sesquiterpene deterrents.
Published in: J Biol Chem

Ligand: JT010 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 9.1899995803833 pEC50
Reference (Journal): A Potent and Site-Selective Agonist of TRPA1.
Published in: J Am Chem Soc

Ligand: (-)-menthol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Primary target: no
Median affinity:  pEC50
Reference (Journal): Bimodal action of menthol on the transient receptor potential channel TRPA1.
Published in: J Neurosci

Ligand: (-)-menthol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of transmembrane domain 5 as a critical molecular determinant of menthol sensitivity in mammalian TRPA1 channels.
Published in: J Neurosci

Ligand: (-)-menthol (Natural product)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Median affinity: 4.2 pIC50
Reference (Journal): More than cool: promiscuous relationships of menthol and other sensory compounds.
Published in: Mol Cell Neurosci

Ligand: methylglyoxal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Inhibiting TRPA1 ion channel reduces loss of cutaneous nerve fiber function in diabetic animals: sustained activation of the TRPA1 channel contributes to the pathogenesis of peripheral diabetic neuropathy.
Published in: Pharmacol Res

Ligand: methylglyoxal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Expression of transient receptor potential ankyrin 1 (TRPA1) and its role in insulin release from rat pancreatic beta cells.
Published in: PLoS ONE

Ligand: methylglyoxal (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Methylglyoxal activates nociceptors through transient receptor potential channel A1 (TRPA1): a possible mechanism of metabolic neuropathies.
Published in: J Biol Chem

Ligand: methyl isocyanate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases.
Published in: FASEB J

Ligand: methyl p-hydroxybenzoate (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 2.4 pEC50
Reference (Journal): Methyl p-hydroxybenzoate causes pain sensation through activation of TRPA1 channels.
Published in: Br J Pharmacol

Ligand: methyl salicylate (Synthetic organic)
Interaction type: Activator
Action: Agonist
Median affinity:  -
Reference (Journal): Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin.
Published in: Neuron

Ligand: morphanthridine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor.
Published in: Toxicol Appl Pharmacol

Ligand: MTSEA (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 2.8 pEC50
Reference (Journal): Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
Published in: Nature

Ligand: N-acetyl-4-benzoquinoneimine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): TRPA1 mediates spinal antinociception induced by acetaminophen and the cannabinoid Δ(9)-tetrahydrocannabiorcol.
Published in: Nat Commun

Ligand: N-acetyl-4-benzoquinoneimine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Acetaminophen, via its reactive metabolite N-acetyl-p-benzo-quinoneimine and transient receptor potential ankyrin-1 stimulation, causes neurogenic inflammation in the airways and other tissues in rodents.
Published in: FASEB J

Ligand: NaHS (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 2.9 pEC50
Reference (Journal): Distribution and function of the hydrogen sulfide-sensitive TRPA1 ion channel in rat urinary bladder.
Published in: Eur Urol

Ligand: NH4Cl (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 2 pEC50
Reference (Journal): Intracellular alkalization causes pain sensation through activation of TRPA1 in mice.
Published in: J Clin Invest

Ligand: nicotine (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 4.800000190734863 pEC50
Reference (Journal): Nicotine activates the chemosensory cation channel TRPA1.
Published in: Nat Neurosci

Ligand: niflumic acid (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Median affinity: 3.3 pEC50
Reference (Journal): Activation of TRPA1 channels by fenamate nonsteroidal anti-inflammatory drugs.
Published in: Pflugers Arch

Ligand: nitrooleic acid (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.7 pEC50
Reference (Journal): Nitrooleic acid, an endogenous product of nitrative stress, activates nociceptive sensory nerves via the direct activation of TRPA1.
Published in: Mol Pharmacol

Ligand: NPPB (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.49 pEC50
Reference (Journal): NPPB structure-specifically activates TRPA1 channels.
Published in: Biochem Pharmacol

Ligand: oleocanthal (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Unusual pungency from extra-virgin olive oil is attributable to restricted spatial expression of the receptor of oleocanthal.
Published in: J Neurosci

Ligand: omega-chloroacetophenone (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.6 pEC50
Reference (Journal): Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor.
Published in: Toxicol Appl Pharmacol

Ligand: O3 (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Ozone activates airway nerves via the selective stimulation of TRPA1 ion channels.
Published in: J Physiol (Lond.)

Ligand: PF-4840154 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Structural insights into the molecular mechanism of mouse TRPA1 activation and inhibition.
Published in: J Gen Physiol

Ligand: PF-4840154 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel.
Published in: Bioorg Med Chem Lett

Ligand: phytocannabinoid 6 [PMID: 38408345] (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV.
Published in: J Nat Prod

Ligand: polygodial (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): TRPA1 mediates the noxious effects of natural sesquiterpene deterrents.
Published in: J Biol Chem

Ligand: prostaglandin A2 (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): Cox-dependent fatty acid metabolites cause pain through activation of the irritant receptor TRPA1.
Published in: Proc Natl Acad Sci USA

Ligand: resolvin D1 (Metabolite)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Resolvin D1 attenuates activation of sensory transient receptor potential channels leading to multiple anti-nociception.
Published in: Br J Pharmacol

Ligand: resolvin D1 (Metabolite)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Resolvin D2 is a potent endogenous inhibitor for transient receptor potential subtype V1/A1, inflammatory pain, and spinal cord synaptic plasticity in mice: distinct roles of resolvin D1, D2, and E1.
Published in: J Neurosci

Ligand: resolvin D2 (Metabolite)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Resolvin D2 is a potent endogenous inhibitor for transient receptor potential subtype V1/A1, inflammatory pain, and spinal cord synaptic plasticity in mice: distinct roles of resolvin D1, D2, and E1.
Published in: J Neurosci

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.5 pIC50
Reference (Journal): Nociceptor and hair cell transducer properties of TRPA1, a channel for pain and hearing.
Published in: J Neurosci

Ligand: salirasib (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Activation of TRPA1 by farnesyl thiosalicylic acid.
Published in: Mol Pharmacol

Ligand: super cinnamaldehyde (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6.1 pEC50
Reference (Journal): Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
Published in: Nature

Ligand: TCS 5861528 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 4.8 pIC50
Reference (Journal): Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals.
Published in: Anesthesiology

Ligand: thymol (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pEC50
Reference (Journal): Thymol and related alkyl phenols activate the hTRPA1 channel.
Published in: Br J Pharmacol

Ligand: URB597 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.599999904632568 pEC50
Reference (Journal): Activation of TRPA1 channels by the fatty acid amide hydrolase inhibitor 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate (URB597).
Published in: Mol Pharmacol

Ligand: Zn2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 2.299999952316284 pEC50
Reference (Journal): Zinc activates damage-sensing TRPA1 ion channels.
Published in: Nat Chem Biol

Ligand: Zn2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 2.299999952316284 pEC50
Reference (Journal): Clioquinol and pyrithione activate TRPA1 by increasing intracellular Zn2+.
Published in: Proc Natl Acad Sci USA