Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPC6

Ligand: 20-HETE (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: 2-APB (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: AM-0883 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Structural basis for pharmacological modulation of the TRPC6 channel.
Published in: Elife

Ligand: AM-1473 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Structural basis for pharmacological modulation of the TRPC6 channel.
Published in: Elife

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 3.9000000953674316 pIC50
Reference (Journal): The transient receptor potential protein homologue TRP6 is the essential component of vascular alpha(1)-adrenoceptor-activated Ca(2+)-permeable cation channel.
Published in: Circ Res

Ligand: arachidonic acid (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: BI 749327 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pIC50
Reference (Journal): In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease.
Published in: Proc Natl Acad Sci U S A

Ligand: BTDM (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Structure of the receptor-activated human TRPC6 and TRPC3 ion channels.
Published in: Cell Res

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Primary target: no
Median affinity: 3.5999999046325684 pIC50
Reference (Journal): The transient receptor potential protein homologue TRP6 is the essential component of vascular alpha(1)-adrenoceptor-activated Ca(2+)-permeable cation channel.
Published in: Circ Res

Ligand: clemizole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pIC50
Reference (Journal): Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5.
Published in: Mol Pharmacol

Ligand: DS88790512 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Published in: Bioorg Med Chem Lett

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

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): The transient receptor potential protein homologue TRP6 is the essential component of vascular alpha(1)-adrenoceptor-activated Ca(2+)-permeable cation channel.
Published in: Circ Res

Ligand: GSK1702934A (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pIC50
Reference (Journal): Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists
Published in: Biophys J

Ligand: GSK2332255B (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy.
Published in: Proc Natl Acad Sci USA

Ligand: GSK2833503A (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy.
Published in: Proc Natl Acad Sci USA

Ligand: GSK417651A (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pIC50
Reference (Journal): The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Published in: Bioorg Med Chem Lett

Ligand: GsMTx-4 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

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

Ligand: hyp 9 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Simple 2,4-diacylphloroglucinols as classic transient receptor potential-6 activators--identification of a novel pharmacophore.
Published in: Mol Pharmacol

Ligand: hyperforin (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Hyperforin--a key constituent of St. John's wort specifically activates TRPC6 channels.
Published in: FASEB J

Ligand: KB-R7943 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: larixyl acetate (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Identification and Validation of Larixyl Acetate as a Potent TRPC6 Inhibitor.
Published in: Mol Pharmacol

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pIC50

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pIC50
Reference (Journal): The transient receptor potential protein homologue TRP6 is the essential component of vascular alpha(1)-adrenoceptor-activated Ca(2+)-permeable cation channel.
Published in: Circ Res

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

Ligand: ML9 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: norgestimate (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 5.28000020980835 pIC50
Reference (Journal): Inhibition of diacylglycerol-sensitive TRPC channels by synthetic and natural steroids.
Published in: PLoS ONE

Ligand: OAG (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol.
Published in: Nature

Ligand: OptoBI-1 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Lipid-independent control of endothelial and neuronal TRPC3 channels by light.
Published in: Chem Sci

Ligand: OptoDArG (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): An optically controlled probe identifies lipid-gating fenestrations within the TRPC3 channel.
Published in: Nat Chem Biol

Ligand: Pyrazolo-pyrimidine 14a [PMID: 29859875] (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Pyrazolo[1,5-a]pyrimidine TRPC6 antagonists for the treatment of gastric cancer.
Published in: Cancer Lett

Ligand: pyrazolopyrimidine 4n (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.860000133514404 pEC50
Reference (Journal): Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
Published in: J Med Chem

Ligand: SAG (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol.
Published in: Nature

Ligand: SAR7334 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.020000457763672 pIC50
Reference (Journal): Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels.
Published in: Br J Pharmacol

Ligand: SH045 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): A (+)-Larixol Congener with High Affinity and Subtype Selectivity toward TRPC6.
Published in: ChemMedChem

Ligand: SKF96365 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): The transient receptor potential protein homologue TRP6 is the essential component of vascular alpha(1)-adrenoceptor-activated Ca(2+)-permeable cation channel.
Published in: Circ Res

Ligand: SLG (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol.
Published in: Nature