Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPM8

Ligand: 2-APB (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
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: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Effects of antagonists and heat on TRPM8 channel currents in dorsal root ganglion neuron activated by nociceptive cold stress and menthol.
Published in: Neurochem Res

Ligand: 5-benzyloxytryptamine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: ACAA (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: AMTB (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome.
Published in: Am J Physiol Renal Physiol

Ligand: anandamide (Metabolite)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: cannabidiol (Natural product)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Primary target: no
Median affinity: 5.550000190734863 pIC50
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: cannabigerol (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
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: cannabigerol (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).
Published in: J Nat Prod

Ligand: cannabigeroquinone (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pIC50
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: capsazepine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  -

Ligand: cooling agent 10 (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Median affinity: 5.2 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: CPS125 (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 4.5 pEC50
Reference (Journal): Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship.
Published in: J Pharm Pharm Sci

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity:  -

Ligand: elismetrep (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pIC50
Reference (Patent): Sulfonamide compounds having trpm8 antagonistic activity

Ligand: eucalyptol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 2.5 pEC50
Reference (Journal): Identification of a cold receptor reveals a general role for TRP channels in thermosensation.
Published in: Nature

Ligand: eucalyptol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 2.1 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: frescolat MGA (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Median affinity: 5.3 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: frescolat ML (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: frescolat ML (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 3.8 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: frescolat ML (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 3.8 pEC50
Reference (Journal): Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship.
Published in: J Pharm Pharm Sci

Ligand: geraniol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 2.2 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: hydroxycitronellal (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 1.7 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): Evolution of thermal response properties in a cold-activated TRP channel.
Published in: PLoS ONE

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): A TRP channel that senses cold stimuli and menthol.
Published in: Cell

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): Identification of a cold receptor reveals a general role for TRP channels in thermosensation.
Published in: Nature

Ligand: icilin (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH.
Published in: J Neurosci

Ligand: isopulegol (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 4.2 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: KPR-5714 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): KPR-5714, a Novel Transient Receptor Potential Melastatin 8 Antagonist, Improves Overactive Bladder via Inhibition of Bladder Afferent Hyperactivity in Rats.
Published in: J Pharmacol Exp Ther

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

Ligand: linalool (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 2.2 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: linoleic acid (Metabolite)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: M8-B (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological blockade of the cold receptor TRPM8 attenuates autonomic and behavioral cold defenses and decreases deep body temperature.
Published in: J Neurosci

Ligand: (+)-menthol (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 4.8 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: (-)-menthol (Natural product)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Primary target: yes
Median affinity: 4.599999904632568 pEC50
Reference (Journal): The principle of temperature-dependent gating in cold- and heat-sensitive TRP channels.
Published in: Nature

Ligand: (-)-menthol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Median affinity:  pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: (-)-menthol (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2008), no prior history available
Median affinity:  pEC50
Reference (Journal): TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH.
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
Median affinity:  pEC50
Reference (Journal): Identification of a cold receptor reveals a general role for TRP channels in thermosensation.
Published in: Nature

Ligand: NADA (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: PBMC (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Pharmacological blockade of TRPM8 ion channels alters cold and cold pain responses in mice.
Published in: PLoS ONE

Ligand: PF-05105679 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.989999771118164 pIC50
Reference (Journal): Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.
Published in: ACS Med Chem Lett

Ligand: phytocannabinoid 6 [PMID: 38408345] (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
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: PMD38 (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Median affinity: 4.5 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: scutellarein (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.769999980926514 pIC50
Reference (Journal): Identification of herbal components as TRPA1 agonists and TRPM8 antagonists.
Published in: J Nat Med

Ligand: tacrolimus (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (1994), EMA (2002)
Primary target: no
Median affinity: 4.849999904632568 pEC50
Reference (Journal): The Immunosuppressant Macrolide Tacrolimus Activates Cold-Sensing TRPM8 Channels.
Published in: J Neurosci

Ligand: thio-BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: thio-BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: thio-BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Contribution of TRPM8 channels to cold transduction in primary sensory neurons and peripheral nerve terminals.
Published in: J Neurosci

Ligand: WS-12 (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship.
Published in: J Pharm Pharm Sci

Ligand: WS-12 (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels.
Published in: Pak J Pharm Sci

Ligand: WS-23 (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 4.4 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: WS-3 (Synthetic organic)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Median affinity: 5.4 pEC50
Reference (Journal): Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Published in: Br J Pharmacol

Ligand: WS-5 (Synthetic organic)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 4.6 pEC50
Reference (Journal): Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship.
Published in: J Pharm Pharm Sci