Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPC5

Ligand: 2-APB (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect.
Published in: Br J Pharmacol

Ligand: AC1903 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.829999923706055 pIC50
Reference (Journal): A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models.
Published in: Science

Ligand: AM12 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): Natural and synthetic flavonoid modulation of TRPC5 channels.
Published in: Br J Pharmacol

Ligand: AM237 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): Potent, selective, and subunit-dependent activation of TRPC5 channels by a xanthine derivative.
Published in: Br J Pharmacol

Ligand: bromoenol lactone (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 4.97 pIC50
Reference (Journal): Bromoenol lactone inhibits voltage-gated Ca2+ and transient receptor potential canonical channels.
Published in: J Pharmacol Exp Ther

Ligand: BTD (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.849999904632568 pEC50
Reference (Journal): A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels.
Published in: Cell Calcium

Ligand: BTD (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pEC50
Reference (Journal): A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels.
Published in: Cell Calcium

Ligand: BTP2 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pEC50

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): Intracellular calcium strongly potentiates agonist-activated TRPC5 channels.
Published in: J Gen Physiol

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): TRPC5 is a Ca2+-activated channel functionally coupled to Ca2+-selective ion channels.
Published in: J Biol Chem

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1957)
Primary target: no
Median affinity:  -

Ligand: clemizole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.960000038146973 pIC50
Reference (Journal): Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5.
Published in: Mol Pharmacol

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

Ligand: (-)-englerin A (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.119999885559082 pEC50
Reference (Journal): (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels.
Published in: Angew Chem Int Ed Engl

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

Ligand: galangin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.349999904632568 pKi
Reference (Journal): Natural and synthetic flavonoid modulation of TRPC5 channels.
Published in: Br J Pharmacol

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

Ligand: genistein (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Genistein potentiates activity of the cation channel TRPC5 independently of tyrosine kinases.
Published in: Br J Pharmacol

Ligand: GFB-8438 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.
Published in: ACS Med Chem Lett

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

Ligand: HC-070 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.029999732971191 pIC50
Reference (Journal): Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice.
Published in: PLoS ONE

Ligand: KB-R7943 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.860000133514404 pIC50
Reference (Journal): The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels.
Published in: Biochem Biophys Res Commun

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

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Lanthanides potentiate TRPC5 currents by an action at extracellular sites close to the pore mouth.
Published in: J Biol Chem

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

Ligand: M084 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.090000152587891 pIC50
Reference (Journal): Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
Published in: J Med Chem

Ligand: M084 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.090000152587891 pIC50
Reference (Journal): Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels.
Published in: Br J Pharmacol

Ligand: methylprednisolone (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1957)
Primary target: no
Median affinity: 4.920000076293945 pEC50
Reference (Journal): A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels.
Published in: Cell Calcium

Ligand: Mg2+ (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 3.34 pIC50
Reference (Journal): A cytosolic residue mediates Mg2+ block and regulates inward current amplitude of a transient receptor potential channel.
Published in: J Neurosci

Ligand: ML204 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
Published in: J Biol Chem

Ligand: Pb2+ (Inorganic)
Interaction type: Activator
Action: None
Primary target: no
Median affinity:  -

Ligand: Pico145 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Picomolar, selective, and subtype-specific small-molecule inhibition of TRPC1/4/5 channels.
Published in: J Biol Chem

Ligand: progesterone (Metabolite)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 5.3 pIC50
Reference (Journal): Stereo-selective inhibition of transient receptor potential TRPC5 cation channels by neuroactive steroids.
Published in: Br J Pharmacol

Ligand: riluzole (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1995), EMA (1996)
Primary target: no
Median affinity: 5.039999961853027 pEC50
Reference (Journal): Riluzole activates TRPC5 channels independently of PLC activity.
Published in: Br J Pharmacol

Ligand: rosiglitazone (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: no
Median affinity: 4.510000228881836 pEC50
Reference (Journal): Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels.
Published in: Mol Pharmacol

Ligand: SKF96365 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: tonantzitlolone (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 pEC50
Reference (Journal): Tonantzitlolone is a nanomolar potency activator of transient receptor potential canonical 1/4/5 channels.
Published in: Br J Pharmacol