Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPV1

Ligand: 12S-HPETE (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances.
Published in: Proc Natl Acad Sci USA

Ligand: 2-APB (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

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

Ligand: 5'-iodoresiniferatoxin (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50

Ligand: 5S-HETE (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: 5S-HPETE (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances.
Published in: Proc Natl Acad Sci USA

Ligand: 6-iodo-nordihydrocapsaicin (Synthetic organic)
Interaction type: Channel blocker
Action: None
Primary target: no
Median affinity: 8 pIC50

Ligand: A-1165442 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Published in: J Med Chem

Ligand: A425619 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.
Published in: J Pharmacol Exp Ther

Ligand: A778317 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Published in: J Pharmacol Exp Ther

Ligand: agatoxin 489 (Natural product)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): An inhibitor of TRPV1 channels isolated from funnel Web spider venom.
Published in: Biochemistry

Ligand: allicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  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: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: AMG517 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Published in: J Med Chem

Ligand: AMG628 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Published in: J Med Chem

Ligand: AMG 9810 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties.
Published in: J Pharmacol Exp Ther

Ligand: anandamide (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide.
Published in: Nature

Ligand: anandamide (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pEC50
Reference (Journal): The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1).
Published in: Br J Pharmacol

Ligand: anandamide (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Activation of TRPV1 by the satiety factor oleoylethanolamide.
Published in: J Biol Chem

Ligand: arvanil (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 9.6 pEC50
Reference (Journal): Cloning and pharmacological characterization of mouse TRPV1.
Published in: Neurosci Lett

Ligand: asivatrep (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 pIC50
Reference (Patent): Compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same

Ligand: AZD1386 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.599999904632568 pIC50
Reference (Webpage): AZD1386 TRPV1 ion channel inhibitor.

Ligand: BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.
Published in: Bioorg Med Chem

Ligand: BCTC (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.
Published in: J Pharmacol Exp Ther

Ligand: camphor (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: capsaicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2009)
Median affinity: 6.1 pEC50
Reference (Journal): The capsaicin receptor: a heat-activated ion channel in the pain pathway.
Published in: Nature

Ligand: capsaicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: yes
Median affinity: 7.5 pEC50
Reference (Journal): The principle of temperature-dependent gating in cold- and heat-sensitive TRP channels.
Published in: Nature

Ligand: capsaicin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2009)
Median affinity: 8 pEC50
Reference (Journal): Cloning and pharmacological characterization of mouse TRPV1.
Published in: Neurosci Lett

Ligand: capsazepine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
Published in: Br J Pharmacol

Ligand: capsazepine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
Published in: Br J Pharmacol

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

Ligand: DkTx (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): A bivalent tarantula toxin activates the capsaicin receptor, TRPV1, by targeting the outer pore domain.
Published in: Cell

Ligand: H+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pEC50

Ligand: JNJ17203212 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Published in: J Med Chem

Ligand: JYL1421 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): High affinity antagonists of the vanilloid receptor.
Published in: Mol Pharmacol

Ligand: LTB4 (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances.
Published in: Proc Natl Acad Sci USA

Ligand: mavatrep (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pIC50
Reference (Journal): Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
Published in: J Med Chem

Ligand: mavatrep (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
Published in: J Med Chem

Ligand: MRS-1477 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.
Published in: J Pharmacol Exp Ther

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

Ligand: olvanil (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 8.4 pEC50
Reference (Journal): Cloning and pharmacological characterization of mouse TRPV1.
Published in: Neurosci Lett

Ligand: olvanil (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 8.1 pEC50
Reference (Journal): Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology.
Published in: Br J Pharmacol

Ligand: olvanil (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology.
Published in: Eur J Pharmacol

Ligand: phenylacetylrinvanil (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Development of the first ultra-potent &quot;capsaicinoid&quot; agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.
Published in: J Pharmacol Exp Ther

Ligand: piperine (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1).
Published in: Br J Pharmacol

Ligand: PPAHV (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
Published in: Br J Pharmacol

Ligand: resiniferatoxin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 9.8 pEC50
Reference (Journal): Cloning and pharmacological characterization of mouse TRPV1.
Published in: Neurosci Lett

Ligand: resiniferatoxin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology.
Published in: Eur J Pharmacol

Ligand: resiniferatoxin (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 7.5 pEC50
Reference (Journal): The capsaicin receptor: a heat-activated ion channel in the pain pathway.
Published in: Nature

Ligand: RhTx (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.28000020980835 pEC50
Reference (Journal): A pain-inducing centipede toxin targets the heat activation machinery of nociceptor TRPV1.
Published in: Nat Commun

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
Published in: Br J Pharmacol

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
Published in: Br J Pharmacol

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

Ligand: SB366791 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist.
Published in: Neuropharmacology

Ligand: SB452533 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKB

Ligand: SB705498 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor.
Published in: J Pharmacol Exp Ther

Ligand: s-RhTx (Peptide)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pEC50
Reference (Journal): Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia.
Published in: Nat Commun

Ligand: [125I]resiniferatoxin (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist.
Published in: Mol Pharmacol

Ligand: [3H]A778317 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]resiniferatoxin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: vanillotoxin-1 (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Spider toxins activate the capsaicin receptor to produce inflammatory pain.
Published in: Nature

Ligand: vanillotoxin-2 (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.87 pEC50
Reference (Journal): Spider toxins activate the capsaicin receptor to produce inflammatory pain.
Published in: Nature

Ligand: vanillotoxin-3 (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 6.35 pEC50
Reference (Journal): Spider toxins activate the capsaicin receptor to produce inflammatory pain.
Published in: Nature

Ligand: zucapsaicin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: Canada (2010)
Primary target: no
Median affinity: 7.550000190734863 pEC50
Reference (Journal): Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.
Published in: J Med Chem