Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPV4

Ligand: 4α-PDD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives.
Published in: J Biol Chem

Ligand: 4α-PDD (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pEC50
Reference (Journal): Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4.
Published in: Br J Pharmacol

Ligand: 5,6-epoxyeicosatrienoic acid (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pEC50
Reference (Journal): Anandamide and arachidonic acid use epoxyeicosatrienoic acids to activate TRPV4 channels.
Published in: Nature

Ligand: AM404 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Modification of TRPV4 activity by acetaminophen.
Published in: Heliyon

Ligand: arachidonic acid (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Anandamide and arachidonic acid use epoxyeicosatrienoic acids to activate TRPV4 channels.
Published in: Nature

Ligand: bisandrographolide (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Bisandrographolide from Andrographis paniculata activates TRPV4 channels.
Published in: J Biol Chem

Ligand: cimifugin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Cimifugin relieves pruritus in psoriasis by inhibiting TRPV4.
Published in: Cell Calcium

Ligand: citric acid (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Impaired pressure sensation in mice lacking TRPV4.
Published in: J Biol Chem

Ligand: Crotamiton (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1955), UK (1997)
Primary target: no
Median affinity:  -
Reference (Journal): Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects.
Published in: Pflugers Arch

Ligand: curcumin (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.179999828338623 pEC50
Reference (Journal): Curcumin Induces Endothelium-Dependent Relaxation by Activating Endothelial TRPV4 Channels.
Published in: J Cardiovasc Transl Res

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: GSK1016790A (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I.
Published in: J Pharmacol Exp Ther

Ligand: GSK1016790A (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 7.7 pEC50
Reference (Journal): N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I.
Published in: J Pharmacol Exp Ther

Ligand: GSK1016790A (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 8 pEC50
Reference (Journal): Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2.
Published in: J Pharmacol Exp Ther

Ligand: GSK2193874 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 8.3 pEC50
Reference (Journal): An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Published in: Sci Transl Med

Ligand: GSK2193874 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 7.4 pEC50
Reference (Journal): An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Published in: Sci Transl Med

Ligand: GSK2193874 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 8.7 pEC50
Reference (Journal): An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Published in: Sci Transl Med

Ligand: GSK2798745 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 pIC50
Reference (Journal): Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Published in: ACS Med Chem Lett

Ligand: GSK-Bz derivative 2b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Discovery and pharmacological characterization of a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moiety.
Published in: Eur J Med Chem

Ligand: HC067047 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
Published in: Proc Natl Acad Sci USA

Ligand: HC067047 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
Published in: Proc Natl Acad Sci USA

Ligand: HC067047 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
Published in: Proc Natl Acad Sci USA

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

Ligand: NSC151066 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 pIC50
Reference (Journal): Structural determinants of TRPV4 inhibition and identification of new antagonists with antiviral activity.
Published in: Br J Pharmacol

Ligand: NSC212069 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.159999847412109 pIC50
Reference (Journal): Structural determinants of TRPV4 inhibition and identification of new antagonists with antiviral activity.
Published in: Br J Pharmacol

Ligand: NSC600684 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Structural determinants of TRPV4 inhibition and identification of new antagonists with antiviral activity.
Published in: Br J Pharmacol

Ligand: paracetamol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1968)
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Modification of TRPV4 activity by acetaminophen.
Published in: Heliyon

Ligand: phorbol 12-myristate 13-acetate (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pEC50
Reference (Journal): Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4.
Published in: Br J Pharmacol

Ligand: phorbol 12-myristate 13-acetate (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives.
Published in: J Biol Chem

Ligand: propofol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 4.409999847412109 pIC50
Reference (Journal): Propofol Induces Cardioprotection Against Ischemia-Reperfusion Injury <i>via</i> Suppression of Transient Receptor Potential Vanilloid 4 Channel.
Published in: Front Pharmacol

Ligand: puerarin (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.769999980926514 pEC50
Reference (Journal): Puerarin induces mouse mesenteric vasodilation and ameliorates hypertension involving endothelial TRPV4 channels.
Published in: Food Funct

Ligand: quinazolin-4(3H) derivative 36 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pEC50
Reference (Journal): Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3 H)-ones and in Vivo Studies on a Surgically Induced Rat Model of Osteoarthritis.
Published in: J Med Chem

Ligand: RN1734 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pIC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN1734 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN1734 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.2 pIC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN1747 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pEC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN1747 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.4 pEC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN1747 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 5.4 pEC50
Reference (Journal): Identification and characterization of novel TRPV4 modulators.
Published in: Biochem Biophys Res Commun

Ligand: RN-9893 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Published in: Bioorg Med Chem Lett

Ligand: RN-9893 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Published in: Bioorg Med Chem Lett

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Heat-evoked activation of the ion channel, TRPV4.
Published in: J Neurosci

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives.
Published in: J Biol Chem

Ligand: vildagliptin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: EMA & UK (2007)
Primary target: no
Median affinity: 3 pEC50
Reference (Journal): Activation of Transient Receptor Potential Channel Vanilloid 4 by DPP-4 (Dipeptidyl Peptidase-4) Inhibitor Vildagliptin Protects Against Diabetic Endothelial Dysfunction.
Published in: Hypertension